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Inhibitors, , Screening Libraries www.MedChemExpress.com

Neuronal Signaling

Neuronal Signaling is involved in the regulation of the mechanics of the central nervous system such as its structure, function, genetics and physiology as well as how this can be applied to understand diseases of the nervous system. Every information processing system in the CNS is composed of and , neurons have evolved unique capabilities for intracellular signaling (communication within the cell) and intercellular signaling (communication between cells). -coupled receptors (GPCRs), including 5-HT , receptor, receptor, and etc, are the largest class of sensory proteins and are important therapeutic targets in Neuronal Signaling. GPCRs are activated by diverse stimuli, including light, enzymatic processing of their N-termini, and binding of proteins, , or small molecules such as , and regulate neuronal excitability by indirectly modulating the function of voltage-gated channels, such as voltage-gated channel and transient receptor potential (TRP) channels. Besides, Notch signaling, such as β- and γ-secretase, also plays multiple roles in the development of the CNS including regulating neural stem cell (NSC) proliferation, survival, self-renewal and differentiation. GPCR dysfunction caused by receptor mutations and environmental challenges contributes to many neurological diseases. Notch signaling in neurons, glia, and NSCs is also involved in pathological changes that occur in disorders such as , Alzheimer's disease and CNS tumors. Thus, targeting Neuronal Signaling, such as notch signaling and GPCRs, can be used as therapeutic interventions for several different CNS disorders.

References: [1] Lathia JD, et al. J Neurochem. 2008 Dec;107(6):1471-81. [2] Palczewski K, et al. Annu Rev Neurosci. 2013 Jul 8;36:139-64.

www.MedChemExpress.com 1 Inhibitors, Agonists, Screening Libraries www.MedChemExpress.com

Target List in Neuronal Signaling

• 5-HT Receptor 3 • Transporter 143

• AChE 27 • γ-secretase 149

• Adenosine Kinase 32

• Amyloid-β 34

• Beta-secretase 40

• CaMK 43

• CGRP Receptor 47

• COMT 50

• Receptor 52

• 67

• FAAH 70

• GABA Receptor 73

• GlyT 84

• iGluR 86

• Imidazoline Receptor 98

• mAChR 100

• Receptor 113

• Receptor 116

• 118

• nAChR 123

• Neurokinin Receptor 129

• 135

2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] 5-HT Receptor Serotonin Receptor;5-hydroxytryptamine Receptor

5-HT receptors (Serotonin receptors) are a group of G protein-coupled receptors (GPCRs) and -gated ion channels (LGICs) found in the central and peripheral nervous systems. Type: 5-HT1, 5-HT2, 5-HT3, 5-HT4, 5-HT5, 5-HT6, 5-HT7. They mediate both excitatory and inhibitory neurotransmission. The serotonin receptors are activated by the serotonin, which acts as their natural ligand. The serotonin receptors modulate the release of many neurotransmitters, as well as many hormones. The serotonin receptors influence various biological and neurological processes such as aggression, , appetite, cognition, learning, , mood, , sleep, andthermoregulation. The serotonin receptors are the target of a variety of pharmaceutical , including many , , ,, gastroprokinetic agents, antimigraine agents, , and entactogens.

www.MedChemExpress.com 3 5-HT Receptor Inhibitors & Modulators

(4E)-SUN9221 (R,R)- Hydrochloride Cat. No.: HY-U00367 Cat. No.: HY-A0021C

Bioactivity: (4E)-SUN9221 is a potent antagonist of α1- receptor Bioactivity: (R,R)-Palonosetron Hydrochloride is the active enantiomer of and 5-HT2 receptor, with antihypertensive and anti-platelet Palonosetron. aggregation activities.

Purity: >98% Purity: 99.61% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 2 mg, 5 mg, 10 mg

(Z)-Thiothixene 5-HT1A modulator 1 Cat. No.: HY-108324 Cat. No.: HY-100290

Bioactivity: (Z)-Thiothixene is an antagonist of receptor Bioactivity: 5-HT1A modulator 1 displays very high affinities for the

extracted from patent US 20150141345 A1. 5HT1A, adrenergic α1 and dopamine D2 receptor with

IC50s of 2 ±0.3 nM, 10 ± 3 nM and 40 ±9 nM, respectively.

Purity: 99.14% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 5 mg, 10 mg, 25 mg

5-HT2 antagonist 1 5-HT2A antagonist 1 Cat. No.: HY-U00365 Cat. No.: HY-U00286

Bioactivity: 5-HT2 antagonist 1 is a potent antagonist of 5-HT2 receptor, Bioactivity: 5-HT2A antagonist 1 is a 5-HT2A antagonist extracted from with weak α1 adrenoceptor blocking activity. patent US5728835A and JP 1007727. 5-HT2A antagonist 1 may be useful in treatment of gastrointestinal disorders circulatory disorders.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

5-HT3 antagonist 1 5-HT3 antagonist 2 Cat. No.: HY-U00368 Cat. No.: HY-U00408

Bioactivity: 5-HT3 antagonist 1 is a potent and selective antagonist of Bioactivity: 5-HT3 antagonist 2 is a 5-HT3 . serotonin 3 (5-HT3) receptor.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

5-HT3-In-1 5-HT4 antagonist 1 Cat. No.: HY-U00413 Cat. No.: HY-100170

Bioactivity: 5-HT3-In-1 is extracted from patent EP0748807A1, compound Bioactivity: 5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a example 8. It shows 5-HT3 inhibition activity. pKi of 9.6.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg

4 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

5-HT6/7 antagonist 1 5-HT7 1 Cat. No.: HY-101622 Cat. No.: HY-109527

Bioactivity: 5-HT6/7 antagonist 1 is a multifunctional ligand that Bioactivity: 5-HT7 agonist 1 is a selective 5-HT7 receptor agonist, with antagonizes 5-HT6/7/2A and D2 receptors, without an IC50 of 222.93 nM, can be used for the 5-HT7 receptor interacting with M1 receptors and hERG channels. related disease, such as CNS disorders.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 250 mg, 500 mg

5HT6-ligand-1 8-OH-DPAT Cat. No.: HY-U00126 (8-Hydroxy-DPAT) Cat. No.: HY-112061

Bioactivity: 5HT6-ligand-1 is a potent 5-HT6 receptor ligand with a Ki of Bioactivity: 8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC of 8.19 for 5-HT1A and a K of 466 nM for 5-HT7; 1.43 nM. 50 i

8-OH-DPAT weakly binds to 5-HT1B (pIC 50, 5.42), 5-HT (pIC

50 <5). Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Abaperidone Adoprazine Cat. No.: HY-101619 (SLV313) Cat. No.: HY-14782

Bioactivity: Abaperidone is a potent antagonist of 5-HT2Areceptor and Bioactivity: Adoprazine, a potential atypical bearing potent D2 receptor antagonist and 5-HT1A receptor agonist properties. dopamine D2 receptor with IC50s of 6.2 and 17 nM.

Purity: >98% Purity: 98.13% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

Agomelatine hydrochloride (S-20098) Cat. No.: HY-17038 (S-20098 hydrochloride) Cat. No.: HY-17038A

Bioactivity: Agomelatine is a competitive antagonist of and porcine Bioactivity: Agomelatine hydrochloride is a , which is serotonin (5-HT2C) receptors (pKi = 6.2 and 6.4, respectively) classified as a -dopamine disinhibitor (NDDI) as well as human 5-HT2B receptors (pKi = 6.6). IC50 value: 6.2 due to its antagonism of the 5-HT2C receptor. (pKi, 5-HT2c); 6.6 (pKi, 5-HT2b) Target: 5-HT2C Receptor; 5-HT2B receptor It is classified as a norepinephrine-dopamine… Purity: 99.88% Purity: 99.49% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Agomelatine L(+)- (S-20098 L(+)-Tartaric acid) Cat. No.: HY-17038B (Alnitidan) Cat. No.: HY-101698

Bioactivity: Agomelatine (L(+)-Tartaric acid) is a antidepressant, which is Bioactivity: Alniditan is a potent 5-HT1B/1D receptors agonist, with classified as a norepinephrine-dopamine disinhibitor (NDDI) IC of 1.7 and 1.3 nM in HEK293 cells, and pK value of 8.96 due to its antagonism of the 5-HT2C receptor. 50 i and 9.40 for 5-HT 1B/1D receptors, respectively.

Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 5

Alosetron ((Z)-2-butenedioate) (GR 68755 (GR 68755; GR 68755X) Cat. No.: HY-70050A ((Z)-2-butenedioate); GR 68755X ((Z)-2-butenedioate)) Cat. No.: HY-70050B

Bioactivity: Alosetron (GR 68755) is a Serotonin 5HT3-receptor antagonist Bioactivity: Alosetron (Z)-2-butenedioate (GR 68755 (Z)-2-butenedioate) is that is used in treatment of irritable bowel syndrome. IC50 a Serotonin 5HT3-receptor antagonist that is used in treatment Value: Target: 5-HT Receptor Alosetron has an antagonist of irritable bowel syndrome. IC50 Value: N/A Target: 5-HT action on the 5-HT3 receptors of the enteric nervous system of Receptor Alosetron has an antagonist action on the 5-HT3 the gastrointestinal tract. While being a 5-HT3 antagonist… receptors of the enteric nervous system of the… Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg Size: 10 mg, 50 mg

Alosetron (Hydrochloride(1:X)) (GR 68755 Alosetron D3 Hydrochloride (Hydrochloride(1:X)); GR 68755X (Hydrochloride(1:X))) Cat. No.: HY-70050 (GR-68755C D3) Cat. No.: HY-70050CS

Bioactivity: Alosetron Hydrochloride(1:X) (GR 68755 Hydrochloride(1:X)) is Bioactivity: Alosetron D3 Hydrochloride (GR-68755C D3) is deuterium labeled a Serotonin 5HT3-receptor antagonist that is used in treatment Alosetron, which is a serotonin 5HT3-receptor antagonist. of irritable bowel syndrome. IC50 Value: N/A Target: 5-HT3 Receptor Alosetron has an antagonist action on the 5-HT3 receptors of the enteric nervous system of the… Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mg, 50 mg Size: 1 mg, 5 mg, 10 mg

Alosetron Hydrochloride (GR 68755C; GR 68755 (Hydrochloride); GR 68755X (Hydrochloride)) Cat. No.: HY-70050C ((RS)-Alprenolol; dl-Alprenolol) Cat. No.: HY-B1517

Bioactivity: Alosetron Hydrochloride (GR 68755 Hydrochloride) is a Bioactivity: Alprenolol is a non-selective as well as 5-HT1A Serotonin 5HT3-receptor antagonist that is used in treatment receptor antagonist. of irritable bowel syndrome. IC50 Value: Target: 5-HT Receptor Alosetron has an antagonist action on the 5-HT3 receptors of the enteric nervous system of the gastrointestinal tract.… Purity: 99.72% Purity: 99.87% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 50 mg, 100 mg

Alprenolol hydrochloride ((RS)-Alprenolol hydrochloride; citrate dl-Alprenolol hydrochloride) Cat. No.: HY-B1517A (NSC 35459) Cat. No.: HY-B0500

Bioactivity: Alprenolol (hydrochloride) is a non-selective beta blocker as Bioactivity: Alverine citrate is a 5-HT1A receptor antagonist, with an well as 5-HT1A receptor antagonist. IC50 of 101 nM.

Purity: 98.98% Purity: 98.71% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 200 mg, 500 mg 5 g, 10 g

AM9405 Ansofaxine hydrochloride Cat. No.: HY-112707 (LY03005; LPM570065) Cat. No.: HY-U00096

Bioactivity: AM9405 is a novel peripherally active type 1 (CB1) Bioactivity: Ansofaxine hydrochloride (LY03005; LPM570065) is a triple and serotonin type 3 receptor agonist. AM9405 inhibits twitch inhibitor; inhibits serotonin, dopamine and

contraction of the ileum and the colon with IC50s of 45.71 and norepinephrine reuptake with IC50 values of 723, 491 and 763 0.076 nM, respectively. nM, respectively.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 500 mg, 250 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 20 mg

6 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

AP521 AR-A 2 Cat. No.: HY-100166 (AR-A 000002) Cat. No.: HY-107018

Bioactivity: AP521 is an agonist of human 5-HT1A receptor with an IC50 Bioactivity: AR-A 2 is a selective 5-HT1B receptor antagonist, with high

of 94 nM. affinity to guinea pig cortex 5HT1B/1D and recombinant

guinea pig 5-HT1B receptors ( Ki=0.24 and 0.47 nM) and with

10-fold lower affinity to guinea pig 5-HT1D receptor ( Ki Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 250 mg, 500 mg

Aripiprazole D8 (OPC-14597) Cat. No.: HY-14546 (OPC-14597 D8) Cat. No.: HY-14546S

Bioactivity: Aripiprazole (OPC-14597) is a human 5-HT1A receptor partial Bioactivity: Aripiprazole D8 (OPC-14597 D8) is the deuterium labeled agonist with a Ki of 4.2 nM. Aripiprazole, which is a human 5-HT1A receptor with a Ki of 4.2 nM.

Purity: 99.98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 100 mg, 200 mg, 500 mg, 1 g

Asenapine hydrochloride (Org 5222) Cat. No.: HY-10121 Cat. No.: HY-16567

Bioactivity: Asenapine(Org 5222) inhibits (α1, α2A, Bioactivity: Asenapine maleate, an antipsychotic, is a 5-HT (1A, 1B, 2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT 2B, , 5A, 6, 7) and Dopamine (D2, D3, D4) receptor receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 antagonist with K values of 0.03-4.0 nM for 5-HT and 1.3, nM. IC50 Value: 0.25-1.2 nM(Ki for adrenergic receptor); i 0.03-4.0 nM(Ki for 5-HT receptor) Target: 5-HT Receptor;… 0.42, 1.1 nM for , respectively. Purity: >98% Purity: 99.39% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

Asenapine maleate AVN-492 (Org 5222 maleate) Cat. No.: HY-11100 Cat. No.: HY-101924

Bioactivity: Asenapine maleate is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) Bioactivity: AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R ( K =91 pM). and D2 antagonist with Ki values of 0.03-4.0 nM, 1.3nM, i respectively, and an antipsychotic.

Purity: 99.95% Purity: 99.49% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Azasetron hydrochloride (Y-25130 hydrochloride) Cat. No.: HY-B0068 (NLX-112; F13640) Cat. No.: HY-14785

Bioactivity: HCl is a selective 5-HT3 receptor antagonist with Bioactivity: Befiradol (NLX-112) is a selective 5-HT1A receptor agonist. IC50 of 0.33 nM used in the management of nausea and induced by cancer chemotherapy.

Purity: 98.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 250 mg, 500 mg 10 mg, 50 mg, 100 mg, 200 mg

www.MedChemExpress.com 7

Befiradol hydrochloride (NLX-112 (hydrochloride); F 13640 (hydrochloride)) Cat. No.: HY-14785A (MDL 72222) Cat. No.: HY-B1541

Bioactivity: Befiradol hydrochloride (NLX-112 hydrochloride) is a selective Bioactivity: Bemesetron (MDL 72222) is a selective 5-HT3 receptor 5-HT1A receptor agonist. [1] antagonist with an IC50 of 0.33 nM . Neuroprotective effect [2].

Purity: 99.22% Purity: 99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 10 mg

Blonanserin (AD-5423) Cat. No.: HY-13575 (OPC-34712) Cat. No.: HY-15780

Bioactivity: (AD-5423) is a D2/5-HT2 receptor antagonist, Bioactivity: Brexpiprazole is a partial agonist of human 5-HT1A and . Target: D2 receptor; 5-HT2 receptor dopamine receptor with Kis of 0.12 nM and 0.3 nM, Blonanserin(AD-5423) is a relatively new atypical respectively. Brexpiprazole is also a 5-HT2A receptor antipsychotic for the treatment of . Blonanserin antagonist with a K of 0.47 nM. belongs to a series of 4-phenyl-2-(1-piperazinyl)pyridines and… i Purity: 99.77% Purity: 99.38% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 25 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

BRL 54443 BRL-15572 dihydrochloride Cat. No.: HY-13221 (BRL-15572) Cat. No.: HY-13200

Bioactivity: BRL 54443 is a potent 5-HT1E/1F receptor agonist (pKi values Bioactivity: BRL-15572 2Hcl is a 5-HT1D receptor antagonist with pKi of are 8.7 and 8.9 respectively); displays > 30-fold 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B selectivity over other 5-HT and dopamine receptors. receptors, exhibiting 60-fold selectivity over 5-HT1B receptor.

Purity: 98.86% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg 10 mg, 50 mg

Bromperidol hydrochloride (R-11333) Cat. No.: HY-B0901 Cat. No.: HY-B1115

Bioactivity: is a derivative, is a potent and Bioactivity: Buspirone hydrochloride is an psychotropic , is long-acting neuroleptic, used as an antipsychotic in the used to treat generalized anxiety disorder (GAD). treatment of schizophrenia.

Purity: 96.36% Purity: 99.64% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg 100 mg

Cariprazine hydrochloride (RGH-188) Cat. No.: HY-14763 (RGH188 hydrochloride) Cat. No.: HY-14763A

Bioactivity: Cariprazine is a novel antipsychotic drug candidate that Bioactivity: Cariprazine hydrochloride is a novel antipsychotic drug

exhibits high affinity for the D3 ( Ki=0.085 nM) and D2 ( candidate that exhibits high affinity for the D3 ( Ki=0.085

Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A nM) and D2 ( Ki=0.49 nM) receptors, and moderate affinity

receptor ( Ki=2.6 nM). for the 5-HT1A receptor ( Ki=2.6 nM). Purity: 99.35% Purity: 99.89% Clinical Data: Launched Clinical Data: Launched Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

8 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Chlorpromazine D6 hydrochloride hydrochloride Cat. No.: HY-B0407AS Cat. No.: HY-B0407A

Bioactivity: Chlorpromazine D6 hydrochloride is the deuterium labeled Bioactivity: Chlorpromazine Hydrochloride is an antagonist of the Chlorpromazine. Chlorpromazine is an inhibitor of dopamine dopamine D2, 5HT2A, and sodium

receptor, 5-HT receptor, potassium channel, . channel. Chlorpromazine binds with D2 and 5HT2A with Kis of 363 nM and 8.3 nM, respectively.

Purity: 99.0% Purity: 99.83% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 1 g, 5 g 1 mg, 5 mg, 10 mg

Cisapride (R 51619; (±)-Cisaprid) Cat. No.: HY-14149 (Clocarpramine; 3-Chlorocarpipramine) Cat. No.: HY-B2073

Bioactivity: (R 51619) is a nonselective 5-HT4 receptor agonist, Bioactivity: Clocapramine is an antagonist of the D2, 5-HT2A it is also a potent hERG potassium channel inhibitor. IC50 receptors. Value: 0.14 μM(EC50 for 5-HT4 receptor) [1]; 9.8 μM (Kv4.3) [2] Target: 5-HT4 Receptor in vitro: Cisapride showed higher inhibitory effects on a hERG current, as indicated by its IC50… Purity: 99.72% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg, 100 mg, 200 mg Size: 1 mg

Clocapramine hydrochloride hydrate N-oxide (3-Chlorocarpipramine hydrochloride hydrate) Cat. No.: HY-B2073A Cat. No.: HY-17366

Bioactivity: Clocapramine hydrochloride hydrate is an antagonist of the Bioactivity: Clozapine N-oxide (CNO) is a major metabolite of the

D2 and 5-HT2A receptors. anti-psychotic drug clozapine. Clozapine N-oxide is a agonist for the chemogenetic Designer Receptors Exclusively Activated by Designer Drug ( DREADD) system.

Purity: >98% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

CP-809101 CP-809101 hydrochloride Cat. No.: HY-15543 Cat. No.: HY-15543A

Bioactivity: CP-809101 is a potent and selective 5-HT2C receptor agonist Bioactivity: CP-809101 Hcl is a potent and selective 5-HT2C receptor with pEC50 of 9.96/7.19/6.81 for human 5-HT2C/5-HT2B/5-HT2A agonist with pEC50 of 9.96/7.19/6.81 for human receptors respectively. 5-HT2C/5-HT2B/5-HT2A receptors respectively.

Purity: >98% Purity: 99.38% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mg, 50 mg Size: 10mM x 1mL in Water, 10 mg, 50 mg

Cyclobenzaprine hydrochloride hydrochloride (MK130 hydrochloride) Cat. No.: HY-B0740 Cat. No.: HY-B0366A

Bioactivity: Hcl is a skeletal and a Bioactivity: Cyproheptadine is a antagonist for 5-HT2 central nervous system (CNS) depressant. receptor with IC50 of 0.6 nM.

Purity: 99.92% Purity: 98.96% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 50 mg, 100 mg, 500 mg, 1 g

www.MedChemExpress.com 9

Cyproheptadine hydrochloride sesquihydrate Cat. No.: HY-B1165 (EGIS-3886) Cat. No.: HY-101630

Bioactivity: Cyproheptadine hydrochloride sesquihydrate is an Bioactivity: Deramciclane has a high affinity for 5-HT2A and 5-HT2C and is an antagonist of serotonin and histamine2. receptors; it acts as an antagonist at both receptor subtypes

and has properties at the 5-HT 2C receptors without direct stimulatory agonist. Purity: 99.20% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 100 mg

Desipramine hydrochloride mesylate Cat. No.: HY-B1272 Cat. No.: HY-B0670A

Bioactivity: hydrochloride is an inhibitor of norepinephrine Bioactivity: Dihydroergotamine mesylate is an ergot used to treat transporter ( NET), 5-HT transporter ( SERT) and migraines.

dopamine transporter ( DAT) with Kis of 4, 61 and 78,720 nM, respectively.

Purity: 99.68% Purity: 99.91% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 10 mg, 50 mg

Dolasetron Mesylate (MDL-73147) Cat. No.: HY-B0750 (MDL-73147EF) Cat. No.: HY-B0750A

Bioactivity: Dolasetron(MDL-73147) is a serotonin 5-HT3 receptor antagonist Bioactivity: Dolasetron Mesylate (MDL-73147EF) is a serotonin 5-HT3 used to treat nausea and vomiting following chemotherapy. receptor antagonist used to treat nausea and vomiting following chemotherapy.

Purity: 98.0% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 5 mg, 10 mg

Dolasetron Mesylate hydrate hydrobromide (MDL-73147EF (hydrate)) Cat. No.: HY-B0750B (Eletriptan HBr) Cat. No.: HY-A0010

Bioactivity: Dolasetron(MDL-73147) is a serotonin 5-HT3 receptor antagonist Bioactivity: Eletriptan HBr is a selective 5-HT1B and 5-HT1D receptor used to treat nausea and vomiting following chemotherapy. agonist with Ki of 0.92 nM and 3.14 nM, respectively. IC50 value: 0.82 nM/3.14 nM (5-HT1B/5-HT1D, Ki) [1] Target: 5-HT1B/5-HT1D in vitro: [3H]Eletriptan has a total number of binding sites (Bmax) of 2478 fmol/mg and 1576 fmol/mg for… Purity: 99.0% Purity: 95.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 200 mg 5 mg, 10 mg, 50 mg, 100 mg

Eltoprazine hydrochloride (DU 28853) Cat. No.: HY-16687 (DU 28853 hydrochloride) Cat. No.: HY-16687A

Bioactivity: Eltoprazine(DU28853) is a serenic or antiaggressive agent Bioactivity: Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor. an antagonist at the 5-HT2C receptor.

Purity: 95.0% Purity: 99.35% Clinical Data: Phase 2 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 10 mg, 50 mg

10 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Eplivanserin mixture (SR-46349) Cat. No.: HY-10792 (SR-46349 (mixture)) Cat. No.: HY-10792A

Bioactivity: Eplivanserin is a potent, selective and orally available Bioactivity: Eplivanserin mixture is a selective serotonin reuptake 5-HT receptor antagonist, with an IC of 5.8 nM in rat 2 50 inhibitor and a 5-HT2A receptor antagonist, extracted from [1] cortical membrane, and a Kd of 1.14 nM. patent WO 2005/002578 A1 .

Purity: >98% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 250 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Eptapirone Eucalyptol (F 11440) Cat. No.: HY-19946 (1,8-Cineole) Cat. No.: HY-N0066

Bioactivity: (F11440) is a potent, selective, high Bioactivity: Eucalyptol is an inhibitor of 5-HT3 receptor , potassium 5-HT1A receptor agonist with marked anxiolytic and channel, TNF-α and IL-1β. antidepressant potential.

Purity: 99.91% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg 50 mg

F-15599 sodium Cat. No.: HY-19863 (Sodium ferulate) Cat. No.: HY-N0060A

Bioactivity: F-15599 is a highly selective G-protein biased 5-HT1A Bioactivity: Ferulic acid (4-hydroxy-3-methoxycinnamic acid) is a phenolic compound present in several plants with claimed beneficial receptor agonist, with Ki of 3.4 nM. effects in prevention and treatment of disorders linked to oxidative stress and inflammation. IC50 value: Target: 5-HT Receptor In vitro: In the present study we have showed that… Purity: >98% Purity: 99.74% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 1 g, 5 g

FK1052 hydrochloride Cat. No.: HY-101638 (BIMT-17; BIMT-17BS) Cat. No.: HY-A0095

Bioactivity: FK1052 hydrochloride is a potent 5-HT3 and 5-HT4 receptor Bioactivity: Flibanserin is a novel multifunctional serotonin agonist and dual antagonist. antagonist (MSAA) that improves sexual functioning in premenopausal women who suffer from reduced sexual interest and desire.

Purity: >98% Purity: 99.31% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Flopropione Cat. No.: HY-100562 (BRL 43694) Cat. No.: HY-B0071

Bioactivity: is a 5-HT1A receptor antagonist and also a Bioactivity: Granisetron (BRL 43694) is a serotonin 5-HT3 receptor catechol-o-methyltransferase ( COMT) inhibitor. antagonist used as an to treat nausea and vomiting following chemotherapy.

Purity: 98.37% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 50 mg, 100 mg 100 mg

www.MedChemExpress.com 11

Granisetron Hydrochloride GSK163090 (BRL 43694A) Cat. No.: HY-B0071A Cat. No.: HY-14348

Bioactivity: Granisetron Hcl(BRL 43694A) is a serotonin 5-HT3 receptor Bioactivity: GSK163090 is a potent, selective, and orally active 5-HT1A/B/D antagonist used as an antiemetic to treat nausea and vomiting receptor antagonist with pKi of 9.4/8.5/9.7, and 6.3/6.7 for following chemotherapy. 5-HT1A/B/D, and dopamine D2/D3, respectively.

Purity: 99.69% Purity: 99.95% Clinical Data: Launched Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Harmine (Telepathine) Cat. No.: HY-N0737A (Lu AE58054) Cat. No.: HY-14338

Bioactivity: is a natural dual-specificity Bioactivity: Idalopirdine (Lu AE58054) is a potent and selective 5-HT6 phosphorylation-regulated kinase ( (DYRK)) inhibitor with receptor antagonist with a Ki of 0.83 nM. anticancer and anti-inflammatory activities.

Purity: 99.78% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg 500 mg

Idalopirdine Hydrochloride (Lu AE58054 (Hydrochloride)) Cat. No.: HY-14338A (HP 873) Cat. No.: HY-17410

Bioactivity: Idalopirdine Hydrochloride (Lu AE58054 Hydrochloride) is a Bioactivity: Iloperidone(HP 873) is a D2/5-HT2 receptor antagonist, which

potent and selective 5-HT6 receptor antagonist with a Ki of is an atypical antipsychotic for the treatment of 0.83 nM. schizophrenia symptoms.

Purity: 99.17% Purity: 99.93% Clinical Data: Phase 3 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 10 mg, 50 mg, 100 mg

Iloperidone hydrochloride (HP 873 hydrochloride) Cat. No.: HY-17410A (SB-742457; GSK-742457; RVT-101) Cat. No.: HY-14339

Bioactivity: Iloperidone (hydrochloride) is a D(2)/5-HT(2) receptor Bioactivity: Intepirdine (SB742457) is a highly selective 5-HT6 receptor antagonistis, which is an atypical antipsychotic for the antagonist with pKi of 9.63; exhibits >100-fold selectivity treatment of schizophrenia symptoms. over other receptors.

Purity: >98% Purity: 98.92% Clinical Data: Launched Clinical Data: Phase 3 Size: 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Irindalone Isocorynoxeine (Lu 21-​098) Cat. No.: HY-101632 (7-Isocorynoxeine) Cat. No.: HY-N0775

Bioactivity: Irindalone is a novel serotonin 5-HT2 antagonist. Bioactivity: Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of 5-HT2A

receptor-mediated current response with an IC50 of 72.4 μM.

Purity: >98% Purity: 99.52% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg

12 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

JNJ-18038683 Cat. No.: HY-19889 (R41468) Cat. No.: HY-10562

Bioactivity: JNJ-18038683 is a 5-Hydroxytryptamine Type 7 ( 5-HT7) Bioactivity: Ketanserin is a selective 5-HT receptor antagonist. Ketanserin also blocks hERG current ( IhERG) in a receptor antagonist, with pKis of 8.19, 8.20 for rat and human concentration-dependent manner ( IC =0.11 μM). 5-HT 7 in HEK293 cells, respectively. 50

Purity: >98% Purity: 98.86% Clinical Data: No Development Reported Clinical Data: Launched Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 50 mg, 100 mg

Ketanserin tartrate (R41468 tartrate) Cat. No.: HY-10562A (COL-144; LY573144) Cat. No.: HY-14861

Bioactivity: Ketanserin tartrate is a selective 5-HT receptor antagonist. Bioactivity: Lasmiditan (COL-144; LY573144) is a high-affinity, highly selective 5-HT1F receptor agonist(Ki=2.1 nM), compared with Ki Ketanserin tartrate also blocks hERG current ( IhERG) in a concentration-dependent manner ( IC =0.11 μM). of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, 50 respectively.

Purity: 99.97% Purity: >98% Clinical Data: Launched Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 2 mg, 5 mg, 10 mg, 50 mg, 100 mg 50 mg, 100 mg

Latrepirdine dihydrochloride dihydrochloride (Dimebolin dihydrochloride) Cat. No.: HY-14537 (E4424) Cat. No.: HY-101609

Bioactivity: dihydrochloride is a neuroactive compound with Bioactivity: Lesopitron dihydrochloride is a full and selective 5-HT1A antagonist activity at , α-adrenergic, and receptor agonist with IC of 125 nM in rat hippocampal serotonergic receptors. Latrepirdine stimulates amyloid 50 precursor protein (APP) catabolism and amyloid-β ( Aβ) membranes. secretion. Purity: 99.75% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg

Lidanserin Lintopride (ZK-33839) Cat. No.: HY-101815 Cat. No.: HY-U00121

Bioactivity: is a drug which acts as a combined 5-HT2A and Bioactivity: Lintopride is a 5HT4 antagonist with moderate 5HT3 antagonist properties. α1-adrenergic receptor antagonist.

Purity: 98.0% Purity: 96.38% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

Loxapine succinate Cat. No.: HY-17390 Cat. No.: HY-17390A

Bioactivity: Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic Bioactivity: Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic receptor antagonist and also a dibenzoxazepine anti-psychotic agent. agent.

Purity: 99.86% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 100 mg, 500 mg

www.MedChemExpress.com 13

LP-211 Tosylate Cat. No.: HY-111455 (ITI-007) Cat. No.: HY-19733

Bioactivity: LP-211 is a selective and blood− barrier penetrant Bioactivity: Lumateperone Tosylate is a 5-HT2A receptor antagonist (Ki =

5-HT7 receptor agonist, with a Ki of 0.58 nM, with high 0.54 nM), a partial agonist of presynaptic D2 receptors and an selectivity over 5-HT receptor (K , 188 nM) and D antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a 1A i 2 SERT blocker (Ki = 61 nM). IC50 value: 0.54 nM (Ki, for 5-HT2A receptor (K , 142 nM). i receptor ) Target: 5-HT2A receptor Lumateperone also possesses… Purity: 99.66% Purity: 99.21% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg 5 mg, 10 mg, 50 mg, 100 mg

Lurasidone Hydrochloride (SM-13496) Cat. No.: HY-B0032A (SM-13496 (Hydrochloride)) Cat. No.: HY-B0032

Bioactivity: Lurasidone (SM-13496) is an antagonist of both dopamine Bioactivity: Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of both dopamine D and 5-HT with IC s of D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, 2 7 50 respectively. Lurasidone (SM-13496) is also a partial agonist 1.68 and 0.495 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist… of 5-HT1A receptor with an IC50 of 6.75 nM. Purity: 99.33% Purity: 99.87% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg, 100 mg Size: 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

LY 344864 LY 344864 hydrochloride Cat. No.: HY-13788 Cat. No.: HY-13788B

Bioactivity: LY344864 is a selective receptor agonist with an affinity of 6 Bioactivity: LY 344864 hydrochloride is a selective 5-HT1F agonist with a nM (Ki) at the recently cloned 5-HT1F receptor. IC50 Value: 6 Ki of 6 nM. nM (Ki) [1] Target: 5-HT1F LY344864 possesses little affinity for the 56 other serotonergic and non-serotonergic neuronal binding sites examined [1]. in vitro: he 5-HT1A, 5-HT1B and… Purity: 99.75% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 5 mg, 10 mg, 50 mg

LY 344864 racemate LY 344864 S-enantiomer Cat. No.: HY-13788C Cat. No.: HY-13788A

Bioactivity: LY 344864 racemate is a 5-HT1F receptor agonist extracted Bioactivity: LY 344864 S-enantiomer is the S-enantiomer of LY344864. from patent US 5708187 A. LY344864 is a 5-HT1F receptor agonist.

Purity: 98.88% Purity: 99.62% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 2 mg, 5 mg

LY310762 LY334370 Cat. No.: HY-13527 Cat. No.: HY-103107

Bioactivity: LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, Bioactivity: LY334370 is a selective 5-HT1F receptor agonist with a Ki of having a weaker affinity for 5-HT1B receptor. 1.6 nM.

Purity: 98.97% Purity: 99.70% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

14 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Metergoline Methiothepin mesylate Cat. No.: HY-B1033 ( mesylate; Ro 8-6837 mesylate) Cat. No.: HY-107836

Bioactivity: is a of the chemical Bioactivity: Methiothepin mesylate is a potent and non-selective 5-HT2 class which acts as a ligand for various serotonin and receptor antagonist, with p K s of 7.10 (5-HT ), 7.28 dopamine receptors. d 1A (5HT 1B), 7.56 (5HT 1C), 6.99 (5HT 1D), 7.0 (5-HT 5A), 7.8

(5-HT 5B), 8.74 (5-HT 6), and 8.99 (5-HT 7), and p Kis… Purity: 99.74% Purity: 99.32% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg 10 mg

MHP 133 Cat. No.: HY-101653 (Org3770; 6-Azamianserin) Cat. No.: HY-B0352

Bioactivity: MHP 133 is a drug with multiple CNS targets, and inhibits Bioactivity: Mirtazapine is a potent antidepressant.

(AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and I2 receptors.

Purity: >98% Purity: 99.77% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 100 mg, 200 mg, 500 mg

Mosapride citrate (TAK-370; AS-4370) Cat. No.: HY-B0189 (TAK-370 citrate; AS-4370 citrate) Cat. No.: HY-B0189A

Bioactivity: Mosapride is a gastroprokinetic agent that acts as a selective Bioactivity: Mosapride citrate is a gastroprokinetic agent that acts as a 5HT4 agonist. selective 5HT4 agonist.

Purity: >98% Purity: 99.74% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

Naftidrofuryl oxalate (Nafronyl oxalate salt) Cat. No.: HY-B1107 (PRX 00023) Cat. No.: HY-14848

Bioactivity: is a drug used in the management of peripheral Bioactivity: Naluzotan is a novel, potent, and selective amidosulfonamide

and cerebral vascular disorders as a vasodilator, enhance 5-HT1A agonist with IC50 and Ki of appr 20 nM and 5.1 nM, cellular oxidative capacity, and may also be a 5-HT2 receptor used for the treatment of anxiety and ; Also a weak antagonist. + hERG K , with IC 50 of 3800 nM. Purity: 97.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 100 mg

NAN-190 hydrobromide Cat. No.: HY-19818A (GR-85548A) Cat. No.: HY-B0197

Bioactivity: NAN-190 hydrobromide is a serotonin receptor 5-HT antagonist. Bioactivity: Naratriptan is a selective 5-HT1 receptor subtype agonist and NAN-190 is a selective antagonist of 5-HT1A. is a drug that is used for the treatment of migraine .

Purity: 99.02% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 10 mg, 50 mg, 100 mg, 200 mg

www.MedChemExpress.com 15

Naratriptan D3 Hydrochloride Naratriptan hydrochloride (GR-85548A D3) Cat. No.: HY-B0197AS (GR-85548A hydrochloride) Cat. No.: HY-B0197A

Bioactivity: Naratriptan D3 Hydrochloride is the deuterium labeled Bioactivity: Naratriptan hydrochloride is a selective 5-HT1 receptor Naratriptan, which is a selective 5-HT1 receptor subtype subtype agonist and is a triptan drug that is used for the agonist. treatment of migraine headaches.

Purity: >98% Purity: 99.65% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

Nefazodone hydrochloride (BMY-13754; MJ-13754-1) Cat. No.: HY-B1396 (APD125) Cat. No.: HY-10559

Bioactivity: hydrochloride is an antidepressant drug. Bioactivity: Nelotanserin is a potent 5-HT2A inverse agonist, a

moderately potent 5-HT2C partial inverse agonist and a weak

5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively. Purity: 99.71% Purity: 99.59% Clinical Data: Launched Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

NEO 376 Nexopamil racemate (SPI-376) Cat. No.: HY-101583 Cat. No.: HY-101727

Bioactivity: NEO 376 is a selective modulator of 5-HT1 receptor, GABA Bioactivity: Nexopamil racemate is the racemate of Nexopamil. Nexopamil is receptor and dopamine receptor, with anti-psychotic 2+ a combined Ca / 5-HT2 antagonist on thrombus formation in actively. vivo and on platelet aggregation in vitro.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

NPS ALX Compound 4a NRA-0160 Cat. No.: HY-103090 Cat. No.: HY-101641

Bioactivity: NPS ALX Compound 4a is a potent and selective Bioactivity: NRA-0160 is a selective dopamine D4 receptor antagonist, 5-hydroxytryptamine (5-HT ) receptor antagonist with an 6 6 with a Ki value of 0.48 nM and with negligible affinity for IC of 7.2 nM, which also has a great binding affinity with 50 dopamine D2 receptor ( Ki: >10000 nM), D3 receptor ( [1] K : 39 nM), rat 5-HT2A receptor ( K : 180 nM) and rat Ki of 0.2 nM . i i Purity: 99.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg

Nuciferine Cat. No.: HY-N0049 (R79598) Cat. No.: HY-101094

Bioactivity: is an antagonist at 5-HT2A ( IC50=478 nM), Bioactivity: Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT2 and dopamine D2 antagonist, and a 5-HT1A 5-HT2C ( IC50=131 nM), and 5-HT2B ( IC50=1 μM), an inverse agonist, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 agonist at 5-HT7 ( IC50=150 nM), a partial agonist at D2 ( nM for 5-HT 2, a 1-adrenergic receptor, dopamine D 2 EC50=64 nM), D5 ( EC50=2.6 μM) and 5-HT6 ( EC50=… Purity: 99.66% Purity: 98.55% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg 5 mg, 10 mg, 50 mg, 100 mg

16 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Olanzapine (LY170053) Cat. No.: HY-14541 (GR 38032; SN 307) Cat. No.: HY-B0002B

Bioactivity: (LY170053) is a high affinity for 5-HT2 serotonin Bioactivity: Ondansetron(GR 38032; SN 307) is a serotonin 5-HT3 receptor and D2 dopamine receptor antagonist. IC50 Value: Target: 5-HT antagonist used mainly as anantiemetic (to treat nausea and Receptor Olanzapine is a that blocks vomiting), often following chemotherapy. IC50 Value: Target: especially the serontonin (5-hydroxytryptamine [5-HT]) 5-HT2A 5- HT3 Receptor in vitro: 5-HT evoked transient inward and the dopamine D2 receptors (Ki values are 4 and 11 nM… currents (EC50 = 3.4 microM; Hill coefficient = 1.8) that were… Purity: 99.94% Purity: 98.55% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg, 100 mg 50 mg, 100 mg, 500 mg

Ondansetron hydrochloride Ondansetron hydrochloride dihydrate (GR 38032 (hydrochloride (GR 38032 (hydrochloride); SN 307 (hydrochloride)) Cat. No.: HY-B0002 dihydrate); SN 307 (hydrochloride dihydrate)) Cat. No.: HY-B0002A

Bioactivity: Ondansetron hydrochloride (GR 38032 hydrochloride; SN 307 Bioactivity: Ondansetron hydrochloride dihydrate (GR 38032 hydrochloride hydrochloride) is a serotonin 5-HT3 receptor antagonist used dihydrate; SN 307 hydrochloride dihydrate) is a serotonin mainly as anantiemetic (to treat nausea and vomiting), often 5-HT3 receptor antagonist used mainly as anantiemetic (to following chemotherapy. Target: 5- HT Receptor IC50 Value: in treat nausea and vomiting), often following chemotherapy. vitro: 5-HT evoked transient inward currents (EC50 = 3.4… Target: 5- HT3 Receptor IC50 Value: in vitro: 5-HT evoked… Purity: >98% Purity: 99.56% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg, 100 mg Size: 50 mg, 100 mg, 1 g, 5 g

Palonosetron Palonosetron Hydrochloride Cat. No.: HY-A0018 Cat. No.: HY-A0021

Bioactivity: Palonosetron is a 5-HT3 antagonist used in the prevention and Bioactivity: Palonosetron Hcl is a 5-HT3 antagonist used in the prevention treatment of chemotherapy-induced nausea and vomiting (CINV). and treatment of chemotherapy-induced nausea and vomiting (CINV).

Purity: >98% Purity: 99.98% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 100 mg Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 200 mg

Pancopride (LAS 30451) Cat. No.: HY-19684 (SLV-308; DU-126891) Cat. No.: HY-14958

Bioactivity: Pancopride is a new potent and selective 5-HT3 receptor Bioactivity: Pardoprunox(SLV-308) is a novel partial dopamine D2 and D3 antagonist. receptor agonist and serotonin 5-HT1A receptor agonist; D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist (IA = 50% and 67%, respectively) and 5-HT1A receptor (pKi = 8.5) full agonist (IA = 100%); also binds to D4 (pKi = 7.8),… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 5 mg, 10 mg, 50 mg, 100 mg

Pardoprunox hydrochloride 401 (SLV-308 hydrochloride; DU-126891 hydrochloride) Cat. No.: HY-14958A Cat. No.: HY-12537

Bioactivity: Pardoprunox hydrochloride is a novel partial dopamine D2 and Bioactivity: Peptide 401, a potent mast cell degranulating factor from bee D3 receptor agonist and serotonin 5-HT1A receptor agonist, D2 venom, suppresses the increased vascular permeability due to (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist and intradermal injection of various spasmogens ( 5-HT1A receptor (pKi = 8.5) full agonist. histamine, and 5-HT).

Purity: 98.89% Purity: 98.29% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 500u g, 1 mg, 5 mg

www.MedChemExpress.com 17

Perphenazine D8 Dihydrochloride Cat. No.: HY-A0077 Cat. No.: HY-A0077AS

Bioactivity: Perphenazine is a drug, inhibits Bioactivity: Perphenazine D8 Dihydrochloride is the deuterium labeled

5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine Perphenazine, which is a typical antipsychotic drug(5-HT, receptor D2/D3, D2L receptor, and , Dopamine receptor ligand).

with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 … Purity: 99.90% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 1 g, 5 g

Phenylbiguanide (N-; PBG; 1-Phenylbiguanide) Cat. No.: HY-101331 (SB-207266) Cat. No.: HY-15574

Bioactivity: Phenylbiguanide is a 5-HT3 receptor selective agonist with Bioactivity: Piboserod (SB 207266) is a selective 5-HT(4) receptor antagonist. an EC50 of 3.0±0.1 μM.

Purity: 98.0% Purity: 98.85% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 10 mg, 50 mg

Piboserod hydrochloride (SB-207266 hydrochloride) Cat. No.: HY-15574A (ACP-103) Cat. No.: HY-14557

Bioactivity: Piboserod (SB 207266) Hcl is a selective 5-HT(4) receptor Bioactivity: Pimavanserin is a selective inverse agonist of the 5-HT2A antagonist. receptor with pIC50 and pKd of 8.73 and 9.3, respectively.

Purity: >98% Purity: 99.73% Clinical Data: Phase 2 Clinical Data: Launched Size: 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

Pimavanserin tartrate (ACP-103 tartrate) Cat. No.: HY-14557A (Pimetixene) Cat. No.: HY-B1101

Bioactivity: Pimavanserin tartrate (ACP-103) is a potent 5-HT 2A receptor Bioactivity: Pimethixene is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene is a highly potent inverse agonist with pIC50 and pKi of 8.73 and 9.3, respectively. antagonist of 5-HT 1A, 5-HT 2A, 5-HT 2B, 5-HT 2C,

histamine H 1, dopamine D 2 and D 4.4 as well as muscari… Purity: 99.50% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

Pimethixene maleate (Pimetixene maleate) Cat. No.: HY-B1101A (LB-46) Cat. No.: HY-B0982

Bioactivity: Pimethixene maleate is antihistamine and antiserotonergic Bioactivity: Pindolol (LB-46) is a nonselective β-blocker with partial compound, acts as an antimigraine agent. Pimethixene maleate beta-adrenergic receptor agonist activity, also functions as a

is a highly potent antagonist of 5-HT 1A, 5-HT 2A, 5-HT 2B, 5-HT1A receptor weak partial agonist / antagonist (Ki=33nM).

5-HT 2C, histamine H 1, dopamine D 2 and D 4.4 as well… Purity: >98% Purity: 99.84% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mg Size: 10mM x 1mL in DMSO, 100 mg

18 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Pizotifen malate (BC-105; Pizotyline) Cat. No.: HY-B0115 (BC-105 (malate); Pizotyline (malate)) Cat. No.: HY-B0115A

Bioactivity: Pizotifen (BC-105) is a potent 5-HT2 receptor antagonist, Bioactivity: Pizotifen (malate) (BC-105 (malate)) is a potent 5-HT2

with a high affinity for 5-HT1C binding site. receptor antagonist, with a high affinity for 5-HT1C binding site.

Purity: 99.65% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg, 200 mg, 500 mg 100 mg, 200 mg, 500 mg

Prucalopride succinate Cat. No.: HY-14151 (R-108512) Cat. No.: HY-12694

Bioactivity: Prucalopride (R093877) is a drug acting as a selective, high Bioactivity: Prucalopride succinate is a selective, high affinity 5-HT4 affinity 5-HT4 receptor agonist(pKi=8.6/8.1 for 5-HT4a/4b); receptor agonist with pKi of 8.6/8.1 for 5-HT4a/4b. >150-fold higher affinity for 5-HT4 receptors than for other receptors. IC50 value: 8.6/8.1 for 5-HT4a/4b(pKi) Target: 5-HT4 receptor Prucalopride is a novel enterokinetic… Purity: 98.0% Purity: 99.97% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 50 mg, 100 mg, 200 mg

PRX-08066 PRX933 hydrochloride Cat. No.: HY-15472 (GW876167 hydrochloride; BVT-933 hydrochloride) Cat. No.: HY-100171

Bioactivity: PRX-08066 is a selective 5-hydroxytryptamine receptor 2B Bioactivity: PRX933 hydrochloride is a 5-HT2c receptor agonist extracted (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective from patent WO 2014140631 A1. vasodilation of pulmonary arteries.

Purity: 97.04% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 5 mg, 10 mg, 25 mg, 50 mg

Puerarin Pumosetrag Hydrochloride Cat. No.: HY-N0145 (MKC-733; DDP-733) Cat. No.: HY-19650

Bioactivity: Puerarin, an isoflavone extracted from Radix puerariae, is a Bioactivity: Pumosetrag Hydrochloride (MKC-733; DDP-733) is an orally 5-HT2C receptor antagonist. available 5-HT3 partial agonist developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease.

Purity: 98.14% Purity: 99.27% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Quetiapine D4 fumarate (ICI204636) Cat. No.: HY-14544 Cat. No.: HY-B0031S

Bioactivity: Quetiapine (ICI204636) is an atypical antipsychotic used in Bioactivity: Quetiapine D4 fumarate is the deuterium labeled Quetiapine, the treatment of schizophrenia, bipolar I mania, bipolar II which is an atypical antipsychotic. depression, bipolar I depression.

Purity: 99.83% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg, 10 mg

www.MedChemExpress.com 19

Quetiapine fumarate Hydrochloride Cat. No.: HY-B0031 (YM060) Cat. No.: HY-B0595

Bioactivity: Quetiapine fumarate is an atypical antipsychotic used in the Bioactivity: Ramosetron Hydrochloride(YM060 Hydrochloride) is a serotonin treatment of schizophrenia, bipolar I mania, bipolar II 5-HT3 receptor antagonist for the treatment of nausea and depression, bipolar I depression. vomiting. Target: 5-HT3 Receptor Ramosetron hydrochloride selectively blocks serotonin receptors (5-HT3). Serotonin plays a vital role in vomiting, serotonin-induced bradycardic… Purity: 99.54 Purity: 99.85% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 10 mg, 50 mg

Revexepride RG-12915 Cat. No.: HY-U00373 Cat. No.: HY-19110

Bioactivity: Revexepride is a highly selective 5-HT4 receptor agonist, Bioactivity: RG-12915 is a selective 5-HT3 antagonist, with IC50 value of and a potential inducer of CYP3A4 , used for the 0.16 nM. treatment of gastroesophageal reflux disease.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

Risperidone hydrochloride (R 64 766) Cat. No.: HY-11018 (R 64 766 hydrochloride) Cat. No.: HY-11018A

Bioactivity: Risperidone is a serotonin 5-HT2 receptor blocker, Bioactivity: Risperidone hydrochloride is a serotonin 5-HT2 receptor

P-Glycoprotein inhibitor and potent dopamine D2 receptor blocker and a potent dopamine D2 receptor antagonist,

antagonist, with Kis of 4.8, 5.9 nM for 5-HT 2A and dopamine with Kis of 0.16, 1.4 nM for 5-HT 2 and D 2 receptor,

D 2 receptor, respectively. respectively. Purity: 99.16% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

Risperidone mesylate (R 64 766 mesylate) Cat. No.: HY-11018B (CYR-101; MIN-101; MT-210) Cat. No.: HY-19469

Bioactivity: Risperidone mesylate(R 64 766 mesylate) is a serotonin 5-HT2 Bioactivity: Roluperidone (CYR-101) is a novel cyclic derivative that

receptor blocker(Ki= 0.16 nM) and a potent dopamine D2 has high equipotent affinities for 5-HT2A and sigma-2 receptor antagonist(Ki= 1.4 nM). receptors ( Ki of 7.53 nM and 8.19 nM for 5-HT 2A and sigma-2, respectively). Purity: >98% Purity: 98.26% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

Rotigotine Rotundine (N-0437; N-0923) Cat. No.: HY-75502 ((-)-; L-Tetrahydropalmatine) Cat. No.: HY-N0096

Bioactivity: is a full agonist of dopamine receptor, a Bioactivity: Rotundine is an antagonist of dopamine D1, D2 and D3

partial agonist of the 5-HT1A receptor, and an antagonist of receptors with IC50s of 166 nM, 1.4 μM and 3.3 μM, the α2B-adrenergic receptor, with Kis of 0.71nM, 4-15nM, and respectively. Rotundine is also an antagonist of 5-HT1A with 83nM for the dopamine D3 receptor and D2, D5, D4 receptors, an IC of 370 nM. and dopamine D1 receptor. 50 Purity: 99.98% Purity: 99.88% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 50 mg

20 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

RS 127445 RU 24969 (MT 500) Cat. No.: HY-15419 Cat. No.: HY-16688

Bioactivity: RS 127445 is a novel high affinity, selective 5-HT2B Bioactivity: RU 24969 is a selective agonist at the 5-HT1A and 5-HT1B receptors. receptor antagonist with pKi of 9.5.

Purity: 99.68% Purity: 99.77% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg

Rupatadine Fumarate (UR-12592) Cat. No.: HY-13511 (UR-12592 (Fumarate)) Cat. No.: HY-13511A

Bioactivity: Rupatadine (UR-12592) is a potent dual PAF/ with Bioactivity: Rupatadine Fumarate (UR-12592 Fumarate) is a potent dual Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet cerebellum membranes). IC50 value: Target: PAF/H1 antagonist membranes/guinea pig cerebellum membranes). IC50 value: in vitro: Rupatadine competitively inhibited histamine-induced Target: PAF/H1 antagonist in vitro: Rupatadine competitively guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without… inhibited histamine-induced guinea pig ileum contraction (pA2… Purity: >98% Purity: 99.34% Clinical Data: Launched Clinical Data: Launched Size: 100 mg, 500 mg Size: 10mM x 1mL in DMSO, 100 mg, 500 mg

Sarpogrelate hydrochloride SB 242084 (MCI-9042) Cat. No.: HY-10564 Cat. No.: HY-13409

Bioactivity: hydrochloride (MCI-9042), a selective 5-HT2 Bioactivity: SB 242084 is a 5-HT2C receptor antagonist(pKi=9.0) that antagonist, has been widely used as an anti-platelet agent for displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B the treatment of PAD. Target: 5-HT2 Recepter Sarpogrelate is a receptors respectively. drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. Sarpogrelate was shown to have the same affinity as… Purity: 98.39% Purity: 99.78% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg

SB 242084 hydrochloride SB 258719 Cat. No.: HY-13409A Cat. No.: HY-U00443

Bioactivity: SB 242084 hydrochloride is a 5-HT2C receptor Bioactivity: SB 258719 is a selective 5-HT7 receptor antagonist with a antagonist(pKi=9.0) that displays 158- and 100-fold pK of 7.5. selectivity over 5-HT2A and 5-HT2B receptors respectively. i IC50 value: 9.0(pKi) [1] Target: 5-HT2C antagonist in vitro: SB 242084 had over 100-fold selectivity over a range of other… Purity: 98.58% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 25 mg 5 mg, 10 mg, 50 mg

SB 271046 Hydrochloride SB-224289 hydrochloride (SB 271046A) Cat. No.: HY-14336A (SB-224289A) Cat. No.: HY-101105A

Bioactivity: SB271046 Hcl is a potent, selective and orally active 5-HT6 Bioactivity: SB-224289 hydrochloride is a selective 5-HT1B receptor receptor antagonist with pKi of 8.9. antagonist, with anxiolytic effect.

Purity: 99.06% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg

www.MedChemExpress.com 21

SB-269970 SB-269970 hydrochloride Cat. No.: HY-15370 (SB-269970A) Cat. No.: HY-15370A

Bioactivity: SB269970 is a 5-HT7 receptor antagonist with pKi of 8.3, Bioactivity: SB269970 hydrochloride is a hydrochloride salt form of exhibits >50-fold selectivity against other receptors. SB-269970, which is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors.

Purity: >98% Purity: 99.41% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

SB-399885 hydrochloride SB-616234A Cat. No.: HY-103099 Cat. No.: HY-19477

Bioactivity: SB-399885 hydrochloride is a 5-HT6 receptor antagonist. Bioactivity: SB-616234A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity.

Purity: 98.93% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Scopolamine hydrobromide ((-)-Scopolamine hydrobromide; (Hyoscine; Scopine (-)-tropate; Scopine tropate) Cat. No.: HY-N0296 Hyoscine hydrobromide; Scopine hydrobromide) Cat. No.: HY-N0296A

Bioactivity: Scopolamine is a high affinity (nM) . Bioactivity: Scopolamine hydrobromide is a high affinity (nM) muscarinic

5-HT3 receptor-responses are reversibly inhibited by antagonist. 5-HT3 receptor-responses are reversibly

Scopolamine with an IC50 of 2.09 μM. inhibited by Scopolamine with an IC50 of 2.09 μM.

Purity: >98% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 100 mg Size: 10mM x 1mL in DMSO, 100 mg, 500 mg

Serotonin hydrochloride (5-Hydroxytryptamine hydrochloride; 5-HT hydrochloride) Cat. No.: HY-B1473 (Lu 23-174) Cat. No.: HY-14543

Bioactivity: Serotonin hydrochloride is a monoamine neurotransmitter in the Bioactivity: Sertindole, a neuroleptic, is one of the newer antipsychotic CNS and an endogenous 5-HT receptor agonist. Serotonin available. Target: Multi-target In vitro studies hydrochloride is also a catechol O-methyltransferase ( showed that sertindole exerts a potent antagonism at serotonin 5-HT2A, 5-HT2C, dopamine D2, and αl adrenergic receptors. COMT) inhibitor with a Ki of 44 μM. Sertindole offers an alternative treatment option for… Purity: 99.97% Purity: 96.14% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg 10 mg, 50 mg

Setiptiline maleate (Org-8282) Cat. No.: HY-32329 (MO-8282) Cat. No.: HY-32329A

Bioactivity: Setiptiline(Org-8282) is a serotonin receptor antagonist. Bioactivity: Setiptiline is a serotonin receptor antagonist.

Purity: 96.00% Purity: 99.89% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

22 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Sulamserod T 82 (RS-100302) Cat. No.: HY-101668 Cat. No.: HY-U00028

Bioactivity: Sulamserod is a 5-HT4 receptor antagonist, with Bioactivity: T 82 is a potent 5-HT3 antagonist and acetylcholinesterase antiarrhythmic activities. (AChE) inhibitor, used for treatment of Alzheimer's Disease.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

Talipexole dihydrochloride (B-HT 920 (dihydrochloride)) Cat. No.: HY-A0008 (SM-3997) Cat. No.: HY-14558

Bioactivity: dihydrochloride (B-HT 920 dihydrochloride) is a Bioactivity: Tandospirone(SM-3997) is a potent and selective 5-HT1A dopamine D2 receptor agonist, α2-adrenoceptor agonist and receptor partial agonist (Ki = 27 nM) that displays 5-HT3 receptor antagonist, which displays antiParkinsonian selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki activity. values ranging from 1300-41000 nM).

Purity: 99.99% Purity: 96.81% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 10 mg, 50 mg, 100 mg

Tandospirone citrate hydrobromide (SM-3997 citrate) Cat. No.: HY-B0061 (Lu AA 24530 hydrobromide) Cat. No.: HY-101755

Bioactivity: Tandospirone citrate is a potent and selective 5-HT1A receptor Bioactivity: Tedatioxetine hydrobromide acts as a triple

partial agonist (Ki = 27 nM) that displays selectivity over and 5-HT2A, 5-HT2C, 5-HT3 and α1A-adrenergic receptor SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki values ranging antagonist. from 1300-41000 nM). IC50 Value: 27±5 nM(Ki) [1] Target: 5-HT1A in vitro: Tandospirone is most potent at the 5-HT1A… Purity: 98.87% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 25 mg

Tegaserod maleate Temanogrel (SDZ-HTF-919; HTF-919) Cat. No.: HY-14153A (APD791) Cat. No.: HY-10560

Bioactivity: maleate is a partial agonist of the 5-HT4 receptor; Bioactivity: Temanogrel is a highly selective 5-HT2A receptor antagonist stimulates the peristaltic reflex and accelerates with a K of 4.9 nM. gastrointestinal transit. i

Purity: 99.80% Purity: 98.14% Clinical Data: Launched Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 1 mg, 5 mg, 10 mg

Tertatolol TG6-10-1 ((±)​-​; Racemic Tertatolol; dl-​Tertatolol) Cat. No.: HY-U00356 Cat. No.: HY-16978

Bioactivity: Tertatolol is a potent antagonist of beta-adrenoceptor and Bioactivity: TG6-10-1 is an EP2 antagonist, shows low-nanomolar antagonist 5-HT receptor, with unique renal vasodilatatory effects. activity against only EP2, >300-fold selectivity over human EP3, EP4, and IP receptors, 100-fold selectivity over EP1 receptors [1].

Purity: >98% Purity: 99.28% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

www.MedChemExpress.com 23

Thioridazine hydrochloride Cat. No.: HY-B0965 Cat. No.: HY-90003

Bioactivity: is an antipsychotic drug, used in the treatment Bioactivity: Tianeptine is a selective facilitator of 5-HT uptake in vitro of schizophrenia and , shows D4 selectivity or and in vivo. IC50 Value: N/A Target: 5-HT Receptor Tianeptine serotonin antagonism. has no affinity for a wide range of receptors, including 5-HT and dopamine (IC50 > 10 μM) and has no effect on noradrenalin or dopamine uptake. Antidepressant, and… Purity: 99.93% Purity: 99.69% Clinical Data: Phase 4 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 5 mg, 10 mg, 50 mg

Tianeptine sodium salt hydrochloride Cat. No.: HY-90003A (AF-1161) Cat. No.: HY-B0478

Bioactivity: Tianeptine sodium salt is a selective facilitator of 5-HT Bioactivity: Trazodone (hydrochloride) (AF-1161) is an antidepressant uptake in vitro and in vivo. IC50 Value: Target: 5-HT Receptor belonging to the class of serotonin receptor antagonists and Tianeptine has no affinity for a wide range of receptors, reuptake inhibitors for treatment of anxiety disorders. including 5-HT and dopamine (IC50 > 10 μM) and has no effect on noradrenalin or dopamine uptake. Antidepressant,… Purity: 99.88% Purity: 99.95% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 100 mg, 500 mg

Trimipramine maleate Cat. No.: HY-B1213 (SDZ-ICS-930 (free base)) Cat. No.: HY-B0072

Bioactivity: maleate is a 5-HT receptor antagonist, with pK is Bioactivity: Tropisetron (SDZ-ICS-930 free base) is a selective 5-HT3 of 6.39, 8.10, 4.66 for 5-HT , 5-HT and 5-HT , receptor antagonist and α7-nicotinic receptor agonist with an 1C 2 1A IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor. IC50 value: 70.1 ± respectively. 0.9 nM [1] Target: 5-HT3 receptor in vitro: Tropisetron specifically inhibited both IL-2 gene transcription and IL-2… Purity: 98.0% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 10 mg, 50 mg, 100 mg

Tropisetron Hydrochloride (SDZ-ICS-930) Cat. No.: HY-B0020 Cat. No.: HY-B0716

Bioactivity: Tropisetron Hydrochloride (SDZ-ICS-930) is a selective 5-HT3 Bioactivity: Urapidil is an α1 adrenoreceptor antagonist and a 5-HT1A receptor antagonist and α7-nicotinic receptor agonist with an receptor agonist. IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor. IC50 value: 70.1 ± 0.9 nM Target: 5-HT3 receptor; α7-nicotinic receptor in vitro: Retinal ganglion cells(RGCs) pretreated with 100 nM… Purity: 99.64% Purity: 99.89% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 50 mg 10 mg, 50 mg, 100 mg

Urapidil hydrochloride hydrochloride Cat. No.: HY-B0354A (SCA 136) Cat. No.: HY-111200

Bioactivity: Urapidil HCl is an α1-adrenoceptor antagonist and 5-HT1A Bioactivity: Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C (

receptor agonist. 5-HT2C) receptor-selective agonist with an EC50 of 8 nM.

Purity: >98% Purity: 98.99% Clinical Data: Launched Clinical Data: No Development Reported Size: 100 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

24 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Vilazodone D8 (EMD 68843; SB659746A) Cat. No.: HY-14262 Cat. No.: HY-14261S

Bioactivity: Vilazodone (EMD 68843; SB 659746A) is a combined serotonin Bioactivity: Vilazodone D8 is the a deuterium labeled vilazodone, which is specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial a combined serotonin specific reuptake inhibitor (SSRI) and agonist currently under clinical evaluation for the treatment 5-HT1A receptor partial agonist. of major depression.

Purity: 99.91% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg 10 mg, 50 mg

Vilazodone Hydrochloride (EMD 68843 (Hydrochloride); SB659746A (Hydrochloride)) Cat. No.: HY-14261 (MDL100907; M 100907) Cat. No.: HY-14940

Bioactivity: Vilazodone Hydrochloride (EMD 68843 Hydrochloride; SB659746A Bioactivity: Volinanserin is a potent and selective antagonist of 5-HT2 Hydrochloride) is a (SER) inhibitor and receptor, with a Ki of 0.36 nM, and shows 300-fold 5-HT1A receptor partial agonist. selectivity for 5-HT 2 receptor over 5-HT 1c, -1 and DA

D 2 receptors. Volinanserin has antipsychotic activity. Purity: 99.94% Purity: 99.71% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg

Vortioxetine hydrobromide (Lu AA 21004) Cat. No.: HY-15414 (Lu AA21004 hydrobromide) Cat. No.: HY-15414A

Bioactivity: Vortioxetine is a inhibitor of 5-HT1A, 5-HT1B, 5-HT3A, Bioactivity: Vortioxetine hydrobromide is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and 5-HT7 receptor and SERT, with Ki values of 15 nM, 33 nM, SERT with K values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 3.7 nM, 19 nM and 1.6 nM, respectively. i nM, respectively. Purity: 98.81% Purity: 99.54% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg

WAY 163909 WAY-100635 Cat. No.: HY-15401 Cat. No.: HY-10349

Bioactivity: WAY 163909 is a potent and selective 5-HT(2C) receptor Bioactivity: WAY-100635 is a potent and selective 5-HT 1A Receptor agonist with a K of 10.5±1.1 nM. i antagonist with a pIC 50 of 8.87, an apparent pA 2 of 9.71.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 5 mg, 10 mg, 50 mg, 100 mg

WAY-100635 Maleate WAY-100635 maleate salt Cat. No.: HY-10349A Cat. No.: HY-13105

Bioactivity: WAY-100635 Maleate is a potent and selective 5-HT 1A Receptor Bioactivity: WAY-100635 maleate salt is a potent and selective antagonist with a pIC of 8.87, an apparent pA of 9.71. 5-hydroxytryptamine1A antagonist with an IC50 of 0.95 ± 0.12 50 2 nM for 5-HT. IC50 Value: 0.95 nM Target: 5-HT Receptor in vitro: WAY 100635 has an IC50 of 1.35 nM and is > 100-fold selective for the 5-HT1A site relative to a range of other CNS… Purity: 98.0% Purity: 99.77% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 25

Wf-516 Xanthotoxol Cat. No.: HY-19417A (8-Hydroxypsoralen) Cat. No.: HY-30152

Bioactivity: Wf-516 is an inhibitor of 5-HT reuptake, and an antagonist Bioactivity: Xanthotoxol is a biologically active linear furocoumarin, shows strong pharmacological activities as anti-inflammatory, of 5-HT1A and 5-HT2A receptors, with Ki of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in , , 5-HT antagonistic, and neuroprotective effects. respectively, and has potent antidepressant activity.

Purity: >98% Purity: 99.15% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg

YL0919 YM348 Cat. No.: HY-100769 Cat. No.: HY-100330

Bioactivity: YL0919, a novel antidepressant candidate with dual activity as Bioactivity: YM348 is a potent and orally active 5-HT2C receptor a 5-HT1A receptor agonist and a selective serotonin reuptake agonist, which shows a high affinity for cloned human 5-HT inhibitor,the IC50 values of YL-0919 inhibiting the uptake of 2C receptor ( K : 0.89 nM). 5-HT into rat cerebral cortical synaptosomes and human i recombinant cells were 1.78±0.34 nM and 1.93±0.18 nM… Purity: 99.84% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

Zatosetron maleate (LY 277359 maleate) Cat. No.: HY-U00234 (CP-88059) Cat. No.: HY-14542

Bioactivity: maleate is a potent and selective 5HT3 receptor Bioactivity: Ziprasidone(CP88059) is a combined 5-HT (serotonin) and antagonist. dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.

Purity: >98% Purity: 98.69% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

Ziprasidone D8 Ziprasidone hydrochloride (CP-88059 D8) Cat. No.: HY-14542S (CP-88059 hydrochloride) Cat. No.: HY-14542A

Bioactivity: Ziprasidone D8 is deuterium labeled Ziprasidone, which is a Bioactivity: Ziprasidone Hcl(CP-88059 Hcl) is a combined 5-HT (serotonin) combined 5-HT (serotonin) and dopamine receptor antagonist and dopamine receptor antagonist which exhibits potent effects which exhibits potent effects of antipsychotic activity. of antipsychotic activity.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mg, 50 mg

Ziprasidone hydrochloride monohydrate (CP 88059 (hydrochloride monohydrate)) Cat. No.: HY-17407

Bioactivity: Ziprasidone hydrochloride monohydrate (CP 88059 hydrochloride monohydrate) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity. Target: 5-HT receptor; Dopamine receptor Ziprasidone hydrochloride monohydrate is the salt… Purity: 99.83% Clinical Data: Launched Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

26 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] AChE Acetylcholinesterase

Acetylcholinesterase (AChE or acetylhydrolase) is a hydrolase that hydrolyzes the neurotransmitter . AChE is found at mainly neuromuscular junctions and brain synapses, where its activity serves to terminate synaptic transmission. It belongs tocarboxylesterase family of . It is the primary target of inhibition by organophosphorus compounds such as nerve agents and . AChE has a very high catalytic activity - each molecule of AChE degrades about 25000 molecules ofacetylcholine (ACh) per second, approaching the limit allowed by diffusion of the substrate. ACh is released from the nerve into the synaptic cleft and binds to ACh receptors on the post-synaptic membrane, relaying the signal from the nerve. AChE, also located on the post-synaptic membrane, terminates the signal transmission by hydrolyzing ACh. The liberated is taken up again by the pre-synaptic nerve and ACh is synthetized by combining with acetyl-CoA through the action of choline acetyltransferase.

www.MedChemExpress.com 27 AChE Inhibitors & Modulators

(+)- (-)- Cat. No.: HY-16009 (Huperzine A) Cat. No.: HY-17387

Bioactivity: (+)-Phenserine is a novel selective Bioactivity: Huperzine A, an active Lycopodium alkaloid extracted from traditional Chinese , is a potent, selective and noncompetitive inhibitor with an IC50 of 45.3 μM. reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD). Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg

(R)- D6 tartrate (±)-Huperzine A Cat. No.: HY-11017AS Cat. No.: HY-17388

Bioactivity: (R)-Rivastigmine D6 (tartrate) is the deuterium labeled Bioactivity: Huperzine A, an active Lycopodium alkaloid extracted from (R)-Rivastigmine, which is an . traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD). IC50 value: Target: AChE Huperzine A exhibited… Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg

4-Methylbenzylidene sulfone (4-MBC; Enzacamene) Cat. No.: HY-17587 Cat. No.: HY-17530

Bioactivity: 4-Methylbenzylidene camphor(4-MBC; Enzacamene)is an organic Bioactivity: Aldicarb sulfone(Temik sulfone) is a ; is camphor derivative that is used in the cosmetic industry for a cholinesterase inhibitor which prevents the breakdown of its ability to protect the skin against UV, specifically UV B acetylcholine in the synapse. radiation.

Purity: 99.98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 100 mg

Benactyzine hydrochloride Benzethonium chloride Cat. No.: HY-B1542A Cat. No.: HY-B0942

Bioactivity: hydrochloride is a ( BChE) Bioactivity: Benzethonium chloride inhibit human recombinant α7 and α4β2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes. inhibitor with a Ki of 0.010 mM.

Purity: 98.74% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 100 mg 100 mg

BuChE-IN-TM-10 (TM-10) Cat. No.: HY-114320 ((+)-Corydaline; Corydalin) Cat. No.: HY-N0923

Bioactivity: BuChE-IN-TM-10 (TM-10) is a potent butyrylcholinesterase Bioactivity: Corydaline is an acetylcholinesterase inhibitor isolated from

(BuChE) inhibitor, with an IC50 of 8.9 nM. BuChE inhibitor 1 Corydalis yanhusuo. inhibits and disaggregates self-induced Aβ aggregation, exhibiting potent antioxidant activity and good blood-brain barrier (BBB) penetration. Has potential to treat Alzheimer’s… Purity: >98% Purity: 98.17% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg

28 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Demecarium (BC-48) Cat. No.: HY-B1626A (E2020 (free base)) Cat. No.: HY-14566

Bioactivity: (BC-48) is a potent cholinesterase Bioactivity: Donepezil(E 2020) is a specific and potent AChE inhibitor for [1] bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM, inhibitor, with an apparent affinity ( Kiapp) of 0.15 μM . respectively. Target: AChE Donepezil is a specific and potent [2] Demecarium Bromide (BC-48) is used as a agent . AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively [1]. Donepezil inhibits the… Purity: 95.0% Purity: 99.87% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg 10 mg, 50 mg, 100 mg

Donepezil Hydrochloride hydrochloride (E2020) Cat. No.: HY-B0034 (Hexahydroadiphenine hydrochloride) Cat. No.: HY-B1239

Bioactivity: Donepezil Hcl(E-2020) is a noncompetitive acetylcholinesterase Bioactivity: Drofenine hydrochloride is a potent competitive inhibitor of inhibitor, which can readily cross the blood brain barrier and BChE, and the ki values of Drofenine is calculated to be 3 uM. increases the concentration of cortical acetylcholine. IC50 value: 3 uM (ki) Target: BChE Benactyzine is widely used drugs, acts on smooth muscle to stop muscle spasms. Purity: 99.97% Purity: 98.10% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 200 mg 50 mg

Edrophonium chloride Epiberberine Cat. No.: HY-B0882 Cat. No.: HY-N0226

Bioactivity: chloride is a readily reversible Bioactivity: Epiberberine is an alkaloid isolated from Coptis chinensis, acts acetylcholinesterase inhibitor; prevents breakdown of the as a potent AChE and BChE inhibitor, and a non-competitive

neurotransmitter acetylcholine and acts by competitively BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, inhibiting the enzyme acetylcholinesterase, mainly at the respectively. Epiberberine has antioxidant activity, w… neuromuscular junction. Purity: 98.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg 100 mg, 500 mg

Epiberberine chloride Galanthamine Cat. No.: HY-N0226A () Cat. No.: HY-76299

Bioactivity: Epiberberine chloride is an alkaloid isolated from Coptis Bioactivity: Galanthamine is a potent acetylcholinesterase ( AChE) chinensis, acts as a potent AChE and BChE inhibitor, and a inhibitor with an IC50 of 500 nM. non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine chloride has antioxid…

Purity: 99.60% Purity: 99.90% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 50 mg, 100 mg

Galanthamine hydrobromide Galanthaminone (Galantamine hydrobromide) Cat. No.: HY-A0009 ((-)-Narwedine; Narwedin) Cat. No.: HY-I0020

Bioactivity: Galanthamine hydrobromide is a long-acting, centrally active Bioactivity: Galanthaminone (Narwedin) is a competitive and reversible acetylcholinesterase(AChE) inhibitor (IC50 = 410 nM) and cholinesterase (AChE) inhibitor; is used for the treatment of allosteric potentiator at neuronal nicotinic ACh receptors. mild to moderate Alzheimer's disease and various other memory IC50 Value: 410 nM Target: AChE Galanthamine hydrobromide impairments. prevents β-amyloid-induced apoptosis in SH-SY5Y and bovine… Purity: 99.93% Purity: 99.53% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 25 mg 100 mg, 500 mg

www.MedChemExpress.com 29

Imperatorin Isoimperatorin (Ammidin) Cat. No.: HY-N0285 Cat. No.: HY-N0286

Bioactivity: Imperatorin is an effective of NO synthesis inhibitor ( Bioactivity: Isoimperatorin is a methanolic extract of the roots of Angelica dahurica shows significant inhibitory effects on IC50=9.2 μmol), which also is a BChE inhibitor ( IC50=31.4 acetylcholinesterase ( AChE) with the IC50 of 74.6 μM. μmol). Imperatorin is a weak agonist of TRPV1 with EC50 of 12.6±3.2 μM. Purity: 98.11% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 25 mg 5 mg, 10 mg, 25 mg, 50 mg

Itopride hydrochloride (HSR803) Cat. No.: HY-B0732 Cat. No.: HY-B0943

Bioactivity: hydrochloride is an AChE inhibitor Bioactivity: Malathion is an parasympathomimetic which (acetylcholinesterase) and D2DR inhibitor. binds irreversibly to cholinesterase, is an insecticide of relatively low human .

Purity: 99.95% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg, 1 g, 5 g 100 mg

Metrifonate MHP 133 (Trichlorfon) Cat. No.: HY-B1220 Cat. No.: HY-101653

Bioactivity: is an irreversible organophosphate Bioactivity: MHP 133 is a drug with multiple CNS targets, and inhibits

acetylcholinesterase inhibitor that is used as an insecticide acetylcholinesterase (AChE) with Ki of 69 μM; also active for the control of flies and roaches. against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.

Purity: 98.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 1 mg, 5 mg, 10 mg, 20 mg 100 mg

Neostigmine methyl sulfate Pitofenone hydrochloride Cat. No.: HY-B1206 Cat. No.: HY-110389

Bioactivity: methyl sulfate is a reversible inhibitor of Bioactivity: Pitofenone hydrochloride, a spasmolytic compound, inhibits the acetylcholinesterase, can not cross the blood-brain barrier. acetylcholinesterase ( AChE) activity from bovine erythrocytes

and from electric eel with Kis of 36 and 45 μM, respectively.

Purity: 99.71% Purity: 99.88% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Pralidoxime chloride hydrochloride (2-PAM chloride) Cat. No.: HY-B1200 Cat. No.: HY-B0949

Bioactivity: chloride is a useful agent in the treatment of Bioactivity: Protriptyline is a antidepressant (TCA), organophosphate poisoning. Pralidoxime binds to specifically a secondary amine, for the treatment of organophosphate-inactivated acetylcholinesterase, used to depression and ADHD. Unique among the TCAs, protriptyline combat poisoning by or acetylcholinesterase tends to be energizing instead of sedating, used for inhibitors (nerve agents) in conjunction with and… narcolepsy to achieve a wakefulness-promoting effect. Purity: 99.0% Purity: 99.91% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 50 mg

30 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Pyridostigmine bromide D6 bromide Cat. No.: HY-B0207A Cat. No.: HY-B0207AS

Bioactivity: Pyridostigmine is a parasympathomimetic and a reversible Bioactivity: Pyridostigmine D6 bromide is the deuterium labeled cholinesterase inhibitor. Target: AChE Pyridostigmine is a Pyridostigmine, which is a parasympathomimetic and a parasympathomimetic and a reversible cholinesterase inhibitor. reversible cholinesterase inhibitor. Since it is a quaternary amine, it is poorly absorbed in the gut and does not cross the blood–brain barrier, except… Purity: 98.0% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 1 g, 5 g 1 mg, 5 mg, 10 mg

Rivastigmine Rivastigmine tartrate (S-Rivastigmine) Cat. No.: HY-17368 (ENA 713; SDZ-ENA 713) Cat. No.: HY-11017

Bioactivity: Rivastigmine, an cholinesterase inhibitor(IC50= 5.5 uM), Bioactivity: Rivastigmine tartrate, an cholinesterase inhibitor(IC50= 5.5 inhibits both butyrylcholinesterase and acetylcholinesterase. uM), inhibits both butyrylcholinesterase and acetylcholinesterase

Purity: 99.39% Purity: 98.53% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 50 mg, 100 mg, 200 mg, 500 mg 50 mg, 100 mg, 200 mg

Scopoletin sn-Glycero-3-phosphocholine (Gelseminic acid; Chrysatropic acid) Cat. No.: HY-N0342 (Choline Alfoscerate; Alpha-GPC; L-α-GPC) Cat. No.: HY-17552

Bioactivity: Scopoletin is an inhibitor of acetylcholinesterase ( AChE). Bioactivity: L-Alpha glycerylphosphorylcholine (alpha-GPC, choline alfoscerate) is a natural choline compound found in the brain and in milk. It is also a parasympathomimetic acetylcholine precursor which may have potential for the treatment of Alzheimer's disease and . IC50 value: Target: Anti-AD… Purity: 99.54% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 50 mg, 100 mg, 200 mg 1 g, 5 g, 10 g

Sophoflavescenol T 82 Cat. No.: HY-N2284 Cat. No.: HY-U00028

Bioactivity: Sophoflavescenol is a prenylated flavonol, which shows great Bioactivity: T 82 is a potent 5-HT3 antagonist and acetylcholinesterase

inhibitory activity with IC50 of 0.013 μM against (AChE) inhibitor, used for treatment of Alzheimer's Disease. Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE,

BACE1, AChE and BChE with IC 50s of 0.30 µM, 0.17 µM, 17… Purity: 98.15% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

Tacrine hydrochloride hydrate Timosaponin AIII Cat. No.: HY-B2244 Cat. No.: HY-N0810

Bioactivity: hydrochloride hydrate is an inhibitor of both acetyl ( Bioactivity: Timosaponin AIII could inhibit acetylcholinesterase (AChE)

AChE) and butyryl-cholinestrase ( BChE) with IC50s of 31 nM activity, with an IC50 of 35.4 μM. and 25.6 nM, respectively.

Purity: 99.98% Purity: 98.88% Clinical Data: Phase 4 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 5 mg, 10 mg, 25 mg

www.MedChemExpress.com 31 Adenosine Kinase ADK

Adenosine kinase (AK) is a cytosolic enzyme that catalyzes the conversion of adenosine to AMP. One potential adenosine regulating agent (ARA) target is adenosine kinase. Adenosine kinase activation represents the major clearance route of adenosine and is partly responsible for its extremely short plasma half-life (<1 s). Inhibition of adenosine kinase results in increased intracellular adenosine which passes out of the cell via passive diffusion or via nucleoside transporter(s) to activate nearby cell-surface adenosine receptors. Thus, adenosine kinase inhibition can represent an alternative mechanism for activation of adenosine receptors and production of adenosine-associated pharmacologies. Adenosine kinase inhibitors (AKIs) represent an alternative strategy, since AKIs may raise local adenosine levels in a more site- and event-specific manner and thereby elicit the desired with a greater therapeutic window. Several potent AKIs are shown to exhibit activity in the rat maximal electric (MES) induced assay.

32 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Adenosine Kinase Inhibitors & Modulators

5-Iodotubercidin ABT-702 dihydrochloride (NSC 113939; 5-ITu) Cat. No.: HY-15424 Cat. No.: HY-103161

Bioactivity: 5-Iodotubercidin is a potent adenosine kinase inhibitor with Bioactivity: ABT-702 dihydrochloride is a potent adenosine kinase ( AK)

IC50 of 26 nM. inhibitor ( IC50=1.7 nM).

Purity: 99.71% Purity: 98.03% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 25 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 33 Amyloid-β β-amyloid peptide;Aβ;Abeta

Amyloid-β (Aβ) denotes peptides of 36–43 amino acids that are crucially involved in Alzheimer's disease as the main component of theamyloid plaques found in the of Alzheimer patients. The peptides result from the amyloid precursor protein (APP), which is being cut by certain enzymes to yield Aβ. Amyloid-β molecules can aggregate to form flexible soluble oligomers which may exist in several forms. Amyloid-β peptide is due to overproduction of Aβ and/or the failure of clearance mechanisms. Amyloid-β self-aggregates into oligomers, which can be of various sizes, and forms diffuse and neuritic plaques in the parenchyma and blood vessels. Amyloid-β oligomers and plaques are potent synaptotoxins, block proteasome function, inhibit mitochondrial activity, alter intracellular Ca2+levels and stimulate inflammatory processes. Loss of the normal physiological functions of Aβ is also thought to contribute to neuronal dysfunction.

34 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Amyloid-β Inhibitors & Modulators

4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine 4-(6-Bromo-2-benzothiazolyl)benzenamine Cat. No.: HY-111513 Cat. No.: HY-111514

Bioactivity: 4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine is a potent Bioactivity: 4-(6-Bromo-2-benzothiazolyl)benzenamine is a β-amyloid PET amyloid imaging agent which binds to Amyloid-β (1-40) with (positron emission tomography) tracer that can be used in the

a KD of 1.7 nM. diagnosis of neurological diseases, such as Alzheimer's and Down's syndrome.

Purity: 98.60% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mg, 50 mg Size: 10 mg, 50 mg

Aftin-4 -peptide(25-35) Cat. No.: HY-111267 (Aβ25-35; β-Amyloid peptide(25-35)) Cat. No.: HY-P0128

Bioactivity: Aftin-4 is an Amyloid-β42 ( Aβ42) inducer. Bioactivity: Amyloid beta-peptide(25-35) is the fragment Aβ(25-35) of the Alzheimer's amyloid β-peptide, has shown neurotoxic activities in cultured cells.

Purity: 98.13% Purity: 98.03% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg amyloid P-IN-1 Amyloid β Peptide (42-1)(human) Cat. No.: HY-19771 Cat. No.: HY-P1362

Bioactivity: pharmaceutical compositions comprising the same and the use of Bioactivity: Amyloid β Peptide (42-1)(human) is the inactive form of the same for treatment of diseases or disorders wherein Amyloid β Peptide (1-42). Amyloid β Peptide (42-1) is a depletion of serum amyloid P component (SAP) would be 42- peptide which plays a key role in the beneficial, including amyloidosis, Alzheimer's disease, type 2 pathogenesis of Alzheimer disease. diabetes mellitus and osteoarthritis. Purity: >98% Purity: 95.13% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Amyloid β-Peptide (1-42) human Amyloid β-Protein 10-20 (β-Amyloid (1-42), human) Cat. No.: HY-P1363 Cat. No.: HY-P1053

Bioactivity: Amyloid β-Peptide (1-42) human is a 42-amino acid peptide Bioactivity: Amyloid β-Protein (10-20) is a fragment of Amyloid-β peptide, which plays a key role in the pathogenesis of Alzheimer maybe used in the research of neurological disease. disease.

Purity: 95.64% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg Size: 1 mg, 5 mg, 10 mg

ARN2966 Beta-Amyloid(1-14),mouse,rat Cat. No.: HY-18292 Cat. No.: HY-P1524

Bioactivity: ARN2966 is a potent post-transcriptional modulator of APP Bioactivity: Beta-Amyloid(1-14),mouse,rat is a 1 to 14 fragment of expression; reduces expression of APP with resultant lower Amyloid-β peptide. production of Aβ.

Purity: 99.57% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 35

BF 227 BF-168 Cat. No.: HY-105252A Cat. No.: HY-112830

Bioactivity: BF 227 is a candidate for an amyloid imaging probe for PET, Bioactivity: BF-168, a candidate probe for PET, is found to specifically

with a Ki of 4.3 nM for Aβ1-42 fibrils. recognize both neuritic and diffuse plaques, with a Ki of 6.4 nM for Aβ1-42.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 250 mg Size: 250 mg, 500 mg

Colivelin Colivelin TFA Cat. No.: HY-P1061 Cat. No.: HY-P1061A

Bioactivity: Colivelin is a neuroprotective peptide and activator of Bioactivity: Colivelin (TFA) is a neuroprotective peptide and activator of STAT3. STAT3.

Purity: >98% Purity: 95.29% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500u g, 1 mg Size: 500u g, 1 mg

Deferoxamine mesylate DWK-1339 (Desferrioxamine B mesylate; DFOM) Cat. No.: HY-B0988 (MDR-1339) Cat. No.: HY-14503

Bioactivity: Deferoxamine mesylate is an iron chelator that binds free iron Bioactivity: DWK-1339 is an orally active and blood-brain-barrier-permeable in a stable complex, preventing it from engaging in chemical Aβ-aggregation inhibitor, used in the research of Alzheimer's reactions. disease.

Purity: 98.0% Purity: 98.97% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Edonerpic maleate FPS-ZM1 (T-817 maleate; T-817MA) Cat. No.: HY-17631A Cat. No.: HY-19370

Bioactivity: Edonerpic maleate is a novel neurotrophic agent which can Bioactivity: FPS-ZM1 is a high-affinity RAGE inhibitor with a Ki of 25 nM. inhibit amyloid-β peptides ( Aβ).

Purity: 99.40% Purity: 99.70% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

Frentizole gamma-Secretase Modulators Cat. No.: HY-15374 (Amyloid-β production inhibitor; γ-Secretase Modulators) Cat. No.: HY-50900

Bioactivity: Frentizole, an FDA-approved immunosuppressive drug, is a novel Bioactivity: gamma-Secretase Modulators (Amyloid-β production inhibitor) is inhibitor of the Aβ-ABAD interaction. a Amyloid-β production inhibitor. gamma-Secretase Modulators is useful for Alzheimer's disease.

Purity: 99.01% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 5 mg, 10 mg

36 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Geniposide Ginsenoside Re Cat. No.: HY-N0009 (Ginsenoside B2; Panaxoside Re; Sanchinoside Re) Cat. No.: HY-N0044

Bioactivity: Geniposide is an iridoid glucoside extracted from Gardenia Bioactivity: Ginsenoside Re (Ginsenoside B2) is an extract from Panax jasminoides Ellis fruits; exhibits a varity of biological notoginseng. Ginsenoside Re decreases the β-amyloid protein activities such as anti-diabetic, antioxidative, ( Aβ). Ginsenoside Re plays a role in antiinflammation antiproliferative and neuroprotective activities. through inhibition of JNK and NF-κB.

Purity: 99.52% Purity: 98.04% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg 5 mg, 10 mg

Ginsenoside Rg1 Ginsenoside Rg2 (Panaxoside A; Panaxoside Rg1) Cat. No.: HY-N0045 (Chikusetsusaponin I; Panaxoside Rg2; Prosapogenin C2) Cat. No.: HY-N0602

Bioactivity: Ginsenoside Rg1 is one of the major active components of Bioactivity: Ginsenoside Rg2 is one of the major active components of . Ginsenoside Rg1 displays promising effects by ginseng. Ginsenoside Rg2 acts as a NF-κB inhibitor.

reducing cerebral Aβ levels. Ginsenoside Rg1 also reduces Ginsenoside Rg2 also reduces Aβ1-42 accumulation. NF-κB nuclear translocation.

Purity: 98.0% Purity: 99.24% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 5 mg, 10 mg

Ginsenoside Rg3 Hoechst 34580 (20(S)-Ginsenoside-Rg3; Rg3; S-Ginsenoside Rg3) Cat. No.: HY-N0603 (HOE 34580) Cat. No.: HY-15560

Bioactivity: Ginsenoside Rg3 is the main component of Red ginseng. Bioactivity: Hoechst 34580 is a cell-permeable fluorescent dye for staining Ginsenoside Rg3 inhibits Na+ and hKv1.4 channel with IC DNA and nuclei.

50s of 32.2±4.5 and 32.6±2.2 μM, respectively. Ginsenoside Rg3 also inhibits Aβ levels, NF-κB activity, and COX-2<… Purity: 98.0% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

Hoechst 34580 tetrahydrochloride K 01-162 (HOE 34580 tetrahydrochloride) Cat. No.: HY-15560B (K162) Cat. No.: HY-14533

Bioactivity: Hoechst 34580 tetrahydrochloride is a cell-permeable Bioactivity: K 01-162 (K162) binds and destabilizes AβO (β-amyloid), with fluorescent dye for staining DNA and nuclei. an EC50 of 80 nM. IC50 value: 80 nM (EC50) Target: Amyloid-β in vitro: The active drug candidate K162 (EC50 = 0.080 μM), stabilizes hydrophobic core I of Aβ42 peptide (residues 17-21) to its α-helical conformation by interacting specifically in… Purity: 99.65% Purity: 99.12% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Latrepirdine dihydrochloride LX2343 (Dimebolin dihydrochloride) Cat. No.: HY-14537 Cat. No.: HY-111383

Bioactivity: Latrepirdine dihydrochloride is a neuroactive compound with Bioactivity: LX2343 is a BACE1 with an IC50 value of antagonist activity at histaminergic, α-adrenergic, and 11.43±0.36 μM. LX2343 acts as a non-ATP competitive PI3K serotonergic receptors. Latrepirdine stimulates amyloid inhibitor with an IC of 15.99±3.23 μM. LX2343 stimulates precursor protein (APP) catabolism and amyloid-β ( Aβ) 50 secretion. autophagy in its promotion of Aβ clearance. Purity: 99.75% Purity: 99.86% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 37

MK-3328 Notoginsenoside R1 Cat. No.: HY-100275 (Sanchinoside R1; Sanqi glucoside R1) Cat. No.: HY-N0615

Bioactivity: MK-3328 is a β-Amyloid PET ligand, which exhibits high Bioactivity: Notoginsenoside R1, the main bioactive component in panaxnotoginseng, is reported have some neuronal protective, binding with an IC50 of 10.5 nM. antihypertensive effects.

Purity: >98% Purity: 97.10% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg

Schisantherin B (Gomisin-B; Wuweizi ester-B; Schisantherin-B) Cat. No.: HY-N0695 (LY450139) Cat. No.: HY-10009

Bioactivity: Schisantherin B (Gomisin-B; Wuweizi ester-B; Schisantherin-B) Bioactivity: Semagacestat is a γ-secretase inhibitor, inhibits is a natural product. β-amyloid ( Aβ42), Aβ38 and Aβ40 with IC50 of 10.9, 12 and 12.1 nM, respectively; also inhibits Notch signaling with

IC50 of 14.1 nM. Purity: >98% Purity: 98.83% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 5 mg, 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Tramiprosate β-Amyloid (1-42), rat (; 3-Amino-1-propanesulfonic acid) Cat. No.: HY-14602 (Amyloid β-peptide (1-42) (rat)) Cat. No.: HY-P1388

Bioactivity: Tramiprosate is a small, orally-administered compound that Bioactivity: β-Amyloid (1-42), rat is a 42-aa peptide, shows cytotoxic binds to soluble Aβ and reduces amyloid aggregation and effect on acute hippocampal slices, and used in the research subsequent deposition target: Aβ In vitro: Tramiprosate of Alzheimer's disease. provides neuroprotection against Aβ-induced in neuronal and mouse organotypic hippocampal cultures, and… Purity: 98.0% Purity: >98% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 500u g, 1 mg, 5 mg 1 g, 5 g

β-Amyloid (1-42), rat TFA β-Amyloid (10-35), amide Cat. No.: HY-P1388A Cat. No.: HY-P1567

Bioactivity: β-Amyloid (1-42), rat TFA is a 42-aa peptide, shows cytotoxic Bioactivity: β-Amyloid (10-35), amide is composed of 26 aa (10-35 residues effect on acute hippocampal slices, and used in the research of the Aβ peptide) and is the primary component of the amyloid of Alzheimer's disease. plaques of Alzheimer’s disease.

Purity: 95.17% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500u g, 1 mg, 5 mg Size: 1 mg, 5 mg, 10 mg

β-amyloid 1-11 β-Amyloid 1-15 Cat. No.: HY-P1510 (Amyloid β-Protein (1-15)) Cat. No.: HY-P1046

Bioactivity: β-amyloid (1-11) is a fragment of Amyloid-β peptide, maybe Bioactivity: β-Amyloid (1-15) is a fragment of β-Amyloid peptide. used in the research of neurological disease. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg

38 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

β-Amyloid 1-16 β-Amyloid 1-17 (Amyloid β-Protein (1-16)) Cat. No.: HY-P1466 Cat. No.: HY-P1772

Bioactivity: β-Amyloid (1-16) is a β-Amyloid protein fragment involved in Bioactivity: β-Amyloid (1-17) is a peptide of β-Amyloid, stabilizes the metal binding. Beta-amyloid is a peptide that forms amyloid fibres and plays a role in Aβ fibre formation [1]. plaques in the brains of Alzheimer's disease (AD) patients.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size:

β-Amyloid 1-28 β-amyloid 12-28 (Amyloid β-Protein (1-28)) Cat. No.: HY-P1468 (Amyloid β-Protein (12-28)) Cat. No.: HY-P1051

Bioactivity: β-Amyloid (1-28) is a β-Amyloid protein fragment involved in Bioactivity: β-amyloid (12-28) is a 17-aa peptide fragment, which can metal binding. Beta-amyloid is a peptide that forms amyloid produce amyloid aggregates, used in the research of plaques in the brains of Alzheimer's disease (AD) patients. Alzheimer’s disease.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg, 10 mg

β-Amyloid 15-21 β-Amyloid 22-35 (Beta-Amyloid (15-21)) Cat. No.: HY-P1521 (Amyloid β-Protein (22-35)) Cat. No.: HY-P1474

Bioactivity: β-amyloid (15-21) is a fragment of Amyloid-β peptide, maybe Bioactivity: β-Amyloid (22-35) is a 14-aa peptide, shows aggregates and used in the research of neurological disease. induces neurotoxicity in the hippocampal cells.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg

β-Amyloid 29-40 β-Amyloid 31-35 (Amyloid beta-protein(29-40)) Cat. No.: HY-P1522 Cat. No.: HY-P1517

Bioactivity: β-Amyloid (29-40) is a fragment of Amyloid-β peptide. Bioactivity: β-Amyloid (31-35) is the shortest sequence of native Amyloid-β peptide that retains neurotoxic activity.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg

β-Amyloid 4-10 Cat. No.: HY-P1787

Bioactivity: β-Amyloid (4-10) is an epitope for the polyclonal anti-Aβ(1-42) antibody, reduces amyloid deposition in a transgenic Alzheimer disease mouse model [1].

Purity: >98% Clinical Data: No Development Reported Size:

www.MedChemExpress.com 39 Beta-secretase BACE;β-Secretase

Beta-secretase (BACE) is an aspartic-acid protease important in the formation of myelin sheaths in peripheral nerve cells. The transmembrane protein contains two active site aspartate residues in its extracellular protein domain and may function as a dimer. Alzheimer's disease (AD) is caused by aggregates of the amyloid peptide (Abeta), which is generated by cleavage of the Abeta protein precursor (APP) by beta-secretase (BACE-1) followed by gamma-secretase. BACE-1 cleavage is limiting for the production of Abeta, Drugs to block this enzyme (BACE inhibitors) prevent the build up of beta-amyloid and may help slow or stop Alzheimers disease.

40 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Beta-secretase Inhibitors & Modulators

AZD3839 free base BACE-1 inhibitor 1 Cat. No.: HY-13438 Cat. No.: HY-112297

Bioactivity: AZD3839 (free base) is a potent and selective BACE1 inhibitor Bioactivity: BACE-1 inhibitor 1 (Compound 8a) is a potent BACE-1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, [1] with an IC50 of 56 nM . also a β-secretase enzyme inhibitor.

Purity: 99.99% Purity: >98% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 100 mg, 250 mg, 500 mg 5 mg, 10 mg, 25 mg, 50 mg

BACE-IN-1 BACE1-IN-1 Cat. No.: HY-U00287 Cat. No.: HY-100182

Bioactivity: BACE-IN-1 (Compound 13) is a substituted lmidazo[1 Bioactivity: BACE1-IN-1 is a potent and highly brain penetrant BACE1 ,2-a]pyridine derivative which can inhibit β-site amyloid inhibitor with IC50s of 32 and 47 nM for human BACE1 and precursor protein-cleaving enzyme (BACE) and that may be BACE2, respectively. useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg

BACE1-IN-2 BACE1-IN-4 Cat. No.: HY-112444 Cat. No.: HY-128594

Bioactivity: BACE1-IN-2 is a 1,4-Oxazine β-Secretase 1 ( BACE1) inhibitor Bioactivity: BACE1-IN-4 is a potent and highly selective BACE1 inhibitor, [1] with an IC of 3.8 nM and a K of 1.9 nM, more selective at with an IC50 of 22 nM . 50 i BACE1 over BACE2. Anti-Alzheimer’s disease [1].

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 250 mg Size: 100 mg, 250 mg, 500 mg

Elenbecestat Epiberberine (E2609) Cat. No.: HY-109055 Cat. No.: HY-N0226

Bioactivity: Elenbecestat (E2609) is a novel potent BACE-1 inhibitor for Bioactivity: Epiberberine is an alkaloid isolated from Coptis chinensis, acts the treatment of Alzheimer's disease (AD) [1]. as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, w…

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 5 mg, 10 mg, 50 mg

Epiberberine chloride Cat. No.: HY-N0226A (BIA 2-093) Cat. No.: HY-B0703

Bioactivity: Epiberberine chloride is an alkaloid isolated from Coptis Bioactivity: Eslicarbazepine acetate, an antiepileptic drug, is a dual a chinensis, acts as a potent AChE and BChE inhibitor, and a dual Inhibitor of β-Secretase and voltage-gated sodium

non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and channel. 8.55 μM, respectively. Epiberberine chloride has antioxid…

Purity: 99.60% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 10 mg, 50 mg, 100 mg, 500 mg

www.MedChemExpress.com 41

Lanabecestat LX2343 (AZD3293; LY3314814) Cat. No.: HY-100740 Cat. No.: HY-111383

Bioactivity: (AZD3293) is a potent, highly permeable, orally Bioactivity: LX2343 is a BACE1 enzyme inhibitor with an IC50 value of active and blood-brain barrier penetrating BACE1 inhibitor 11.43±0.36 μM. LX2343 acts as a non-ATP competitive PI3K with a Ki of 0.4 nM. inhibitor with an IC50 of 15.99±3.23 μM. LX2343 stimulates autophagy in its promotion of Aβ clearance. Purity: 99.76% Purity: 99.86% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

LY2811376 LY2886721 Cat. No.: HY-10472 Cat. No.: HY-13240

Bioactivity: LY2811376 is the first orally available non-peptidic Bioactivity: LY2886721 is an BACE inhibitor used for the treatment of

β-secretase (BACE1) inhibitor with IC50 of 239 nM-249 nM, Alzheimer's Disease.

that acts to decrease Aβ secretion with EC50 of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 o… Purity: 99.79% Purity: 99.67% Clinical Data: Phase 1 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

PF-06751979 Sophoflavescenol Cat. No.: HY-112157 Cat. No.: HY-N2284

Bioactivity: PF-06751979 is a potent, brain penetrant, β-site amyloid Bioactivity: Sophoflavescenol is a prenylated flavonol, which shows great

precursor protein cleaving enzyme 1 ( BACE1) inhibitor with inhibitory activity with IC50 of 0.013 μM against an IC 50 of 7.3 nM in BACE1 binding assay. Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE,

BACE1, AChE and BChE with IC 50s of 0.30 µM, 0.17 µM, 17… Purity: 99.00% Purity: 98.15% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Umibecestat (CNP520) Cat. No.: HY-119689 (MK-8931) Cat. No.: HY-16759

Bioactivity: Umibecestat (CNP520) is a beta-site amyloid precursor protein Bioactivity: Verubecestat (MK-8931) is a beta-secretase 1 (BACE1)

cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and inhibitor under investigation for the treatment of Alzheimer's Disease. 10 nM for human BACE-1 and mouse BACE-1, respectively [1].

Purity: >98% Purity: 99.79% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

β-Secretase Inhibitor IV (Axon 1125) Cat. No.: HY-10133

Bioactivity: β-Secretase Inhibitor IV is a potent, cell-active BACE-1

inhibitor with IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively.

Purity: >98% Clinical Data: No Development Reported Size: 250 mg, 500 mg

42 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] CaMK Calmodulin-dependent protein kinases;Calmodulin-dependent kinases

The Ca2+/calmodulin-dependent kinase (CaMK) family has been recognized as a key mediator in living organisms and various biological processes. Calcium/calmodulin kinase II (CaMK II) is a multifunctional cytoplasmic calcium and calmodulin-dependent protein kinase that phosphorylates and alters the function of a variety of substrates. The CaMK II pathway has been found to regulate the RANKL-induced osteoclast formation via the cAMP-response element binding protein (CREB) pathway. Among many signaling pathways of proliferation, intracellular calciumol/L has been extensively demonstrated to be very important. In cytoplasm, calciumol/L binds to calmodulin, and then activates the Ca2+/calmodulin (CaM) dependent kinases (CaMKs) which are a family of structurally related / protein kinases including CaMKI-IV. CaMKII, a multi functional protein kinase, is ubiquitously involved in many physiological processes including control of cell cycle, apoptosis, gene expression, and neurotransmission.

www.MedChemExpress.com 43 CaMK Inhibitors & Modulators

A-484954 Autocamtide 2 Cat. No.: HY-110096 (Autocamtide II) Cat. No.: HY-P0225

Bioactivity: A-484954 is a highly selective eukaryotic elongationfactor-2 Bioactivity: Autocamtide 2 is a highly selective peptide substrate of

(eEF2) inhibitor, with an IC50 of 280 nM. calcium/calmodulin-dependent protein kinase II ( CaMKII). It can be used in the CaMKII activity assay.

Purity: 98.01% Purity: 98.17% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg 5 mg, 10 mg, 25 mg, 50 mg

Autocamtide 2, amide Autocamtide-2-related inhibitory peptide TFA Cat. No.: HY-P1528 Cat. No.: HY-P0214A

Bioactivity: Autocamtide 2, amide is a substrate (100 μM final Bioactivity: Autocamtide-2-related inhibitory peptide (TFA) is a highly

concentration) for CaMK family assays. specific and potent inhibitor of CaMKII with an IC50 of 40 nM.

Purity: >98% Purity: 98.48% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg

Calmidazolium chloride Calmodulin-Dependent Protein Kinase II 290-309 (R 24571) Cat. No.: HY-103319 Cat. No.: HY-P1479

Bioactivity: Calmidazolium chloride (R 24571) is a calmodulin (CaMK) Bioactivity: Calmodulin-Dependent Protein Kinase II (290-309) is a potent

antagonist, antagonizing CaM-dependent phosphodiesterase and CaMK antagonist with an IC50 of 52 nM for inhibition of Ca calmodulin-induced activation of erythrocyte Ca2+-transporting 2+/calmodulin-dependent protein kinase II. [1] ATPase with IC50s of 0.15 and 0.35 μM, respectively . A… Purity: 99.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg Size: 1 mg, 5 mg

CaMKII-IN-1 DDD107498 succinate Cat. No.: HY-18271 (DDD-498 succinate) Cat. No.: HY-117684A

Bioactivity: CaMKII-IN-1 is a potent and highly selective CaMKII inhibitor Bioactivity: DDD107498 succinate (DDD-498 succinate) is a potent and orally with IC50 of 63 nM; significantly high selectivity against active antimalarial agent, inhibits multiple life-cycle

CaMKIV, MLCK, p38a, Akt1, and PKC. stages of the parasite, with an EC50 of 1 nM against P. falciparum 3D7. DDD107498 succinate inhibits prot…

Purity: 98.09% Purity: 98.72% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

KN-62 KN-92 Cat. No.: HY-13290 Cat. No.: HY-15517

Bioactivity: KN-62 is a selective and potent inhibitor of Bioactivity: KN-92 is an inactive derivative of KN-93. KN-93 is a selective

calmodulin-dependent protein kinase II ( CaMK-II) with IC50 inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), of 0.9 μM, KN-62 also displays noncompetitive antagonism at competitively blocking CaM binding to the kinase (Ki = 370 nM). P2X7 receptors in HEK293 cells, with an IC50 value… Purity: 99.16% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 2 mg, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg

44 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

KN-92 hydrochloride KN-92 phosphate Cat. No.: HY-15517B Cat. No.: HY-15517A

Bioactivity: KN-92 is an inactive derivative of KN-93. KN-93 is a selective Bioactivity: KN-92 is an inactive derivative of KN-93. KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 competitively blocking CaM binding to the kinase (Ki = 370 nM). nM). IC50 value: Target: KN-92 is intended to be used as a control compound in studies designed to elucidate the… Purity: 99.77% Purity: 99.94% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 2 mg, 5 mg, 10 mg, 50 mg 2 mg, 5 mg, 10 mg, 50 mg

KN-93 KN-93 hydrochloride Cat. No.: HY-15465 Cat. No.: HY-15465A

Bioactivity: KN-93 is a cell-permeable, reversible and competitive Bioactivity: KN-93 hydrochloride is a cell-permeable, reversible and inhibitor calmodulin-dependent kinase type II ( CaMKII) competitive inhibitor calmodulin-dependent kinase type II (

with a Ki of 370 nM. CaMKII) with a Ki of 370 nM.

Purity: 98.79% Purity: 99.67% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

KN-93 phosphate Metofenazate Cat. No.: HY-15465B (Methophenazine) Cat. No.: HY-100263

Bioactivity: KN-93 phosphate is a novel membrane-permeant synthetic Bioactivity: Metofenazate is a selective calmodulin inhibitor.

inhibitor of purified neuronal CaMK-II, with K i of 370 nM.

Purity: 99.97% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 1 mg, 5 mg, 10 mg 1 mg, 5 mg, 10 mg, 50 mg

MLCK inhibitor peptide 18 NH125 Cat. No.: HY-P1029 Cat. No.: HY-100576

Bioactivity: MLCK inhibitor peptide 18 is a myosin light chain kinase ( Bioactivity: NH125 is a potent and selective inhibitor of eukaryotic

MLCK) inhibitor with an IC50 of 50 nM, and inhibits CaM elongation factor 2 kinase (eEF-2K/CaMKIII), also could induce eEF2 phosphorylation, with an IC of 60 nM for eEF-2K. kinase II only at 4000-fold higher concentrations. 50

Purity: 98.71% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 25 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Rimacalib STO-609 (SMP 114) Cat. No.: HY-100779 Cat. No.: HY-19805

Bioactivity: Rimacalib is a Ca 2+/calmodulin-dependent protein kinase II Bioactivity: STO-609 is a selective and cell-permeable inhibitor of the Ca 2+ (CaMKII) inhibitor, with IC50s of ~1 μM for CaMKIIα to ~30 /calmodulin-dependent protein kinase kinase ( CaM-KK), μM for CaMKIIγ. with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. STO-609 inhibits AMP-activated prot… Purity: 98.75% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

www.MedChemExpress.com 45

Syntide 2 Cat. No.: HY-P0271

Bioactivity: Syntide 2 is recognized as a substrate by Ca 2+/calmodulin-dependent protein kinase II ( CaMKII) with

a Ki of 12 μM.

Purity: >98% Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg

46 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] CGRP Receptor Calcitonin gene-related peptide receptor

CGRP receptor is a heterotrimer: a large peptide with 7 transmembrane domains, named calcitonin receptor-like receptor (CLR or CRLR), is supplemented by a small single transmembrane peptide, named receptor activity-modifying protein (RAMP1) that forms the CGRP-specific ligand binding site. CGRP receptors are expressed by multiple different cell types within the nervous, cardiovascular and immune systems that are thought to play important roles in migraine pathology: on cerebral vascular smooth muscle, where they cause vasodilation, on dural mast cells triggering their degranulation, at the central terminals of the trigeminal nerve, where CGRP is a neuromodulator at second-order nociceptive neurons in the spinal trigeminal nucleus caudalis and in the dorsal horn of the spinal cord, where CGRP has a similar role in inducing central sensitisation to tactile stimuli. CGRP is produced in both peripheral and central neurons. It is a potent peptide vasodilator and can function in the transmission of pain.

www.MedChemExpress.com 47 CGRP Receptor Inhibitors & Modulators

Adrenomedullin (1-50), rat Adrenomedullin (11-50), rat Cat. No.: HY-P1534 Cat. No.: HY-P1766

Bioactivity: Adrenomedullin (1-50), rat is a 50 amino acid peptide, which Bioactivity: Adrenomedullin (11-50), rat is the C-terminal fragment (11-50) induces a selective arterial vasodilation via activation of of rat adrenomedullin. Rat adrenomedullin induces a selective CGRP1 receptor. arterial vasodilation via CGRP1 receptors [1].

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500u g, 1 mg, 5 mg Size:

Adrenomedullin (16-31), human Adrenomedullin (AM) (22-52), human Cat. No.: HY-P1770 (22-52-Adrenomedullin (human)) Cat. No.: HY-P1471

Bioactivity: Adrenomedullin (16-31), human is amino acid residues 16-31 Bioactivity: Adrenomedullin (AM) (22-52), human is an adrenomedullin fragment of human adrenomedullin (hADM). Adrenomedullin has receptor antagonist, and also antagonizes the calcitonin appreciable affinity for the CGRP1 receptor. Adrenomedullin generelated peptide ( CGRP) receptor in the hindlimb vascular (16-31), human possesses pressor activity in the systemic bed of the cat. vascular bed of the rat, but not the cat [1]. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size: 500u g, 1 mg, 5 mg

Calcitonin Gene Related Peptide (CGRP) (83-119), rat Calcitonin Gene Related Peptide (CGRP) (83-119), rat TFA Cat. No.: HY-P1462 Cat. No.: HY-P1462A

Bioactivity: Calcitonin Gene Related Peptide (CGRP) (83-119), rat is a 37 Bioactivity: Calcitonin Gene Related Peptide (CGRP) (83-119), rat (TFA) is amino acid calcitonin family of neuropeptide, acts through a 37 amino acid calcitonin family of neuropeptide, acts calcitonin receptor-like receptor ( CRLR). through calcitonin receptor-like receptor ( CRLR).

Purity: >98% Purity: 96.21% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500u g, 1 mg, 5 mg Size: 500u g, 1 mg, 5 mg

CGRP antagonist 1 HCGRP-(8-37) Cat. No.: HY-112262 (Human α-CGRP (8-37)) Cat. No.: HY-P1014

Bioactivity: CGRP antagonist 1 is a highly potent CGRP receptor Bioactivity: HCGRP-(8-37) is a human calcitonin gene-related peptide (hCGRP) fragment and also an antagonist of CGRP receptor. antagonist with a Ki and IC50 of 35 and 57 nM, respectively.

Purity: >98% Purity: 98.28% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 500u g, 1 mg, 5 mg

MK-3207 MK-3207 Hydrochloride Cat. No.: HY-10301 Cat. No.: HY-10302

Bioactivity: MK-3207 is a potent and orally bioavailable CGRP receptor Bioactivity: MK-3207 (Hydrochloride) is a potent and orally bioavailable

antagonist (IC50= 0.12 nM; Ki value= 0.024 nM); highly CGRP receptor antagonist with IC50 of 0.12 nM and Ki of selective versus human AM1, AM2, CTR, and AMY3. IC50 Value: 0.024 nM, and is highly selective versus human AM1, AM2, CTR, 0.024 nM (Ki, Human CGRP) [1] In common with other CGRP and AMY3. receptor antagonists, MK-3207 displays lower affinity for… Purity: 98.76% Purity: 98.07% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 5 mg, 10 mg, 50 mg, 100 mg

48 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Olcegepant Olcegepant hydrochloride (BIBN-4096; BIBN 4096BS) Cat. No.: HY-10095 (BIBN-4096 hydrochloride; BIBN4096BS hydrochloride) Cat. No.: HY-10095A

Bioactivity: Olcegepant is a potent and selective non-peptide antagonist of Bioactivity: Olcegepant hydrochloride is the first potent and selective the calcitonin gene-related peptide 1 (CGRP1) receptor with non-peptide antagonist of the calcitonin gene-related peptide 1

IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP. (CGRP1) receptor with IC50 of 0.03 nM and with a Ki of 14.4 pM for human CGRP.

Purity: 99.32% Purity: 99.31% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 2 mg, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg

Rat CGRP-(8-37) Rimegepant Cat. No.: HY-P0209 (BMS-927711) Cat. No.: HY-15498

Bioactivity: Rat CGRP-(8-37) (VTHRLAGLLSRSGGVVKDNFVPTNVGSEAF) is a Bioactivity: Rimegepant (BMS-927711) is a highly potent, oral calcitonin

highly selective CGRP receptor antagonist. gene-related peptide ( CGRP) receptor antagonist with a Ki value of 0.027 nM.

Purity: 98.29% Purity: 99.08% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 500u g, 1 mg, 5 mg Size: 5 mg, 10 mg, 50 mg, 100 mg

Telcagepant Ubrogepant (MK-0974) Cat. No.: HY-32709 (MK-1602) Cat. No.: HY-12366

Bioactivity: Telcagepant (MK-0974) is a calcitonin gene-related peptide Bioactivity: Ubrogepant (MK-1602) is a novel oral calcitonin gene-related peptide receptor ( CGRP) antagonist in development for acute (CGRP) receptor antagonist with Kis of 0.77 nM and 1.2 nM for [1] human and rhesus CGRP receptors, respectively. treatment of migraine .

Purity: 99.07% Purity: >98% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

β-CGRP, human β-CGRP, human TFA (Human β-CGRP; CGRP-II (Human)) Cat. No.: HY-P1548 (Human β-CGRP (TFA); CGRP-II (Human) (TFA)) Cat. No.: HY-P1548A

Bioactivity: β-CGRP, human is one of calcitonin peptides, acts via the Bioactivity: β-CGRP, human TFA is one of calcitonin peptides, acts via the complex of calcitonin-receptor-like receptor (CRLR) and complex of calcitonin-receptor-like receptor (CRLR) and

receptor-activity-modifying protein (RAMP), with IC50s of 1 nM receptor-activity-modifying protein (RAMP), with IC50s of 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2 in cells. and 300 nM for CRLR/RAMP1 and CRLR/RAMP2 in cells [1]. Purity: >98% Purity: 98.82% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500u g, 1 mg, 5 mg Size: 500u g, 1 mg, 5 mg

www.MedChemExpress.com 49 COMT Catechol-O-methyltransferase

Catechol O-methyltransferase (COMT) is a ubiquitous bisubstrate -dependent enzyme found in plants, animals and microorganisms. COMT catalyses the transfer of a methyl group from S-adenosyl-L-methionine (SAM) to one of the hydroxyl oxygen atoms (preferentially the 3-hydroxyl) in a catechol substrate. Physiological substrates of COMT are catecholamine neurotransmitters such as dopamine, noradrenaline, and their metabolites. COMT also methylates catecholic steroids such as 2-hydroxyestradiol as well as a range of other catecholic compounds including neuroactive drugs such as L-dopa, α- and isoproterenol. COMT inhibition is a means of treating Parkinson’s disease, schizophrenia and depression. There are two isoforms of human COMT: soluble cytoplasmic COMT (S-COMT), which is mainly intracellular, and a membrane-bound form (MB-COMT), which has a single-span helix contained within a 50 amino acid extension at the N-terminus. COMT is an enzyme that plays a major role in catechol neurotransmitter deactivation. Inhibition of COMT can increase neurotransmitter levels, which provides a means of treatment for Parkinson’s disease, schizophrenia and depression.

50 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] COMT Inhibitors & Modulators

Entacapone sodium salt Cat. No.: HY-14280 Cat. No.: HY-14280A

Bioactivity: Entacapone is a specific, potent, peripherally acting Bioactivity: Entacapone is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment. IC50 Value: 151 nM Target: COMT in vitro: nM for PD treatment. Entacapone inhibits catechol-O-methyltransferase(COMT) with similar IC50 in different tissues including live, duodenum,… Purity: 99.97% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

Flopropione Cat. No.: HY-100562 (BIA 9-1067) Cat. No.: HY-14896

Bioactivity: Flopropione is a 5-HT1A receptor antagonist and also a Bioactivity: Opicapone is an available catechol-O-methyltransferase ( catechol-o-methyltransferase ( COMT) inhibitor. COMT) inhibitor. Opicapone decreases the ATP content of the cells with IC 50 values of 98 μM.

Purity: 98.37% Purity: 99.60% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg 100 mg

Serotonin hydrochloride (5-Hydroxytryptamine hydrochloride; 5-HT hydrochloride) Cat. No.: HY-B1473 (Ro 40-7592) Cat. No.: HY-17406

Bioactivity: Serotonin hydrochloride is a monoamine neurotransmitter in the Bioactivity: Tolcapone(Ro 40-7592) is an orally active selective, potent CNS and an endogenous 5-HT receptor agonist. Serotonin catechol-O-methyltransferase (COMT) inhibitor. hydrochloride is also a catechol O-methyltransferase (

COMT) inhibitor with a Ki of 44 μM.

Purity: 99.97% Purity: 99.52% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 51 Dopamine Receptor

Dopamine Receptors are a class of G protein-coupled receptors that are prominent in the vertebrate central nervous system (CNS). The neurotransmitter dopamine is the primary endogenous ligand for dopamine receptors. Dopamine receptors are implicated in many neurological processes, including motivation, pleasure, cognition, memory, learning, and fine motor control, as well as modulation of neuroendocrine signaling. Abnormal dopamine receptor signaling and nerve function is implicated in several neuropsychiatric disorders. Thus, dopamine receptors are common neurologic drug targets; antipsychotics are often dopamine receptor antagonists while psychostimulants are typically indirect agonists of dopamine receptors. There are at least five subtypes of dopamine receptors, D1, D2, D3, D4, and D5. The D1 and D5 receptors are members of the D1-like family of dopamine receptors, whereas the D2, D3 and D4receptors are members of the D2-like family.

52 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Dopamine Receptor Inhibitors & Modulators

(+)- hydrochloride (+)-PD 128907 hydrochloride (DAR-0100 hydrochloride) Cat. No.: HY-101299 Cat. No.: HY-110000

Bioactivity: (+)-Dihydrexidine hydrochloride is a dopamine D1 receptor Bioactivity: (+)-PD 128907 hydrochloride is a selective dopamine D2/D3 agonist with an EC50 of 72± 21 nM. receptor agonist, with Kis of 1.7, 0.84 nM for human and rat D

3 receptors, 179, 770 n M for human and rat D 3 receptors, respectively. Purity: >98% Purity: 98.83% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg

(±)-Methotrimeprazine (D6) 5-HT6/7 antagonist 1 (dl-Methotrimeprazine D6) Cat. No.: HY-19489S Cat. No.: HY-101622

Bioactivity: (±)-Methotrimeprazine (D6) is the deuterium labeled Bioactivity: 5-HT6/7 antagonist 1 is a multifunctional ligand that Methotrimeprazine, which is a D3 dopamine and Histamine H1 antagonizes 5-HT6/7/2A and D2 receptors, without receptor antagonist. interacting with M1 receptors and hERG channels.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg Size: 250 mg, 500 mg

A-381393 A-437203 Cat. No.: HY-116941 (Lu201640; A37203) Cat. No.: HY-U00185

Bioactivity: A-381393 is a potent, selective, brain penetrate dopamine Bioactivity: A-437203 is a selective D3 receptor antagonist with Ki of D receptor antagonist, with K s of 1.5, 1.9 and 1.6 nM for 4 i 71, 1.6, and 6220 nM for D 2, D 3, and D 4 receptors, human dopamine D 4.4, D 4.2, and D 4.7 receptor, respectively.

respectively, >2700-fold selectivity over D 1, D 2, D 3 Purity: 99.96% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg 5 mg, 10 mg, 25 mg, 50 mg

Abaperidone ABT-670 Cat. No.: HY-101619 Cat. No.: HY-19483

Bioactivity: Abaperidone is a potent antagonist of 5-HT2Areceptor and Bioactivity: ABT-670 is a selective, oral bioavailable agonist of dopamine D4 receptor, with EC50 of 89 nM, 160 nM, and dopamine D2 receptor with IC50s of 6.2 and 17 nM. 93 nM for humanD 4, ferretD 4, and ratD 4, respectively.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

Adoprazine hydrochloride (SLV313) Cat. No.: HY-14782 Cat. No.: HY-A0125A

Bioactivity: Adoprazine, a potential atypical antipsychotic bearing potent Bioactivity: Alizapride hydrochloride is a dopamine receptor antagonist D2 receptor antagonist and 5-HT1A receptor agonist properties. with prokinetic and antiemetic effects which can also be used in the treatment of nausea and vomiting, including postoperative nausea and vomiting.

Purity: 98.13% Purity: 99.95% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 50 mg, 100 mg

www.MedChemExpress.com 53

Amisulpride hydrochloride (DAN 2163) Cat. No.: HY-14545 (DAN 2163 hydrochloride) Cat. No.: HY-14545A

Bioactivity: Amisulpride is a dopamine D2/D3 receptor antagonist with Bioactivity: Amisulpride hydrochloride is a dopamine D2/D3 receptor

Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, antagonist with Kis of 2.8 and 3.2 nM for human dopamine

respectively. D2 and D3, respectively.

Purity: 98.0% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 100 mg, 200 mg, 500 mg Size: 100 mg, 200 mg, 500 mg

Asenapine hydrochloride Cat. No.: HY-16567 (R-1929) Cat. No.: HY-B1470

Bioactivity: Asenapine maleate, an antipsychotic, is a 5-HT (1A, 1B, 2A, Bioactivity: Azaperone (R-1929) acts as a but also has some antihistaminic and anticholinergic properties. Azaperone 2B, 2C, 5A, 6, 7) and Dopamine (D2, D3, D4) receptor antagonist with K values of 0.03-4.0 nM for 5-HT and 1.3, is a pyridinylpiperazine and butyrophenone neuroleptic drug i with and antiemetic effects, which is used mainly as 0.42, 1.1 nM for Dopamine receptor, respectively. a tranquilizer in veterinary medicine. Purity: 99.39% Purity: 99.58% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 100 mg, 500 mg

Benzamide Derivative 1 Blonanserin Cat. No.: HY-U00415 (AD-5423) Cat. No.: HY-13575

Bioactivity: Derivative 1 is a benzamide derivative from patent Bioactivity: Blonanserin(AD-5423) is a D2/5-HT2 receptor antagonist, EP0213775A1, compound 18. Benzamide Derivative 1 may be useful atypical antipsychotic. Target: D2 receptor; 5-HT2 receptor in treatment of gastrointestinal disorders. Blonanserin(AD-5423) is a relatively new atypical antipsychotic for the treatment of schizophrenia. Blonanserin belongs to a series of 4-phenyl-2-(1-piperazinyl)pyridines and… Purity: >98% Purity: 99.77% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 10 mg, 25 mg, 100 mg

BP 897 Brexpiprazole Cat. No.: HY-106660 (OPC-34712) Cat. No.: HY-15780

Bioactivity: BP 897 is a potent and selective dopamine D3 receptor Bioactivity: Brexpiprazole is a partial agonist of human 5-HT1A and

agonist, and a weak dopamine D2 receptor antagonist, with dopamine receptor with Kis of 0.12 nM and 0.3 nM, K s of 0.92 nM and 61 nM for D3 and D2 receptors, and shows i respectively. Brexpiprazole is also a 5-HT2A receptor

low affinities at D1 and D4 receptors ( Kis, 3 and 0.3… antagonist with a Ki of 0.47 nM. Purity: >98% Purity: 99.38% Clinical Data: No Development Reported Clinical Data: Launched Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

Bromocriptine mesylate (CB-154) Cat. No.: HY-12705A Cat. No.: HY-B1164

Bioactivity: mesylate is a potent dopamine D2/D3 receptor Bioactivity: Bromopride is a dopamine antagonist with prokinetic

agonist, which binds D2 dopamine receptor with pKi of properties widely used as an antiemetic. 8.05±0.2.

Purity: 99.98% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg 50 mg, 100 mg, 200 mg

54 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Cabergoline Cariprazine (FCE-21336) Cat. No.: HY-15296 (RGH-188) Cat. No.: HY-14763

Bioactivity: is an ergot derived-dopamine D 2-like receptor Bioactivity: Cariprazine is a novel antipsychotic drug candidate that exhibits high affinity for the D ( K =0.085 nM) and D ( agonist that has high affinity for D2, D3, and 5-HT2B 3 i 2 K =0.49 nM) receptors, and moderate affinity for the 5-HT receptors ( Ki=0.7, 1.5, and 1.2, respectively). i 1A receptor ( Ki=2.6 nM). Purity: 99.90% Purity: 99.35% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg

Cariprazine hydrochloride CGP 25454A (RGH188 hydrochloride) Cat. No.: HY-14763A Cat. No.: HY-100454

Bioactivity: Cariprazine hydrochloride is a novel antipsychotic drug Bioactivity: CGP 25454A is a novel and selective presynaptic dopamine

candidate that exhibits high affinity for the D3 ( Ki=0.085 autoreceptor antagonist.

nM) and D2 ( Ki=0.49 nM) receptors, and moderate affinity

for the 5-HT1A receptor ( Ki=2.6 nM). Purity: 99.89% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

Chlorpromazine D6 hydrochloride Chlorpromazine hydrochloride Cat. No.: HY-B0407AS Cat. No.: HY-B0407A

Bioactivity: Chlorpromazine D6 hydrochloride is the deuterium labeled Bioactivity: Chlorpromazine Hydrochloride is an antagonist of the Chlorpromazine. Chlorpromazine is an inhibitor of dopamine dopamine D2, 5HT2A, potassium channel and sodium

receptor, 5-HT receptor, potassium channel, sodium channel. channel. Chlorpromazine binds with D2 and 5HT2A with Kis of 363 nM and 8.3 nM, respectively.

Purity: 99.0% Purity: 99.83% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 1 g, 5 g 1 mg, 5 mg, 10 mg

Chlorprothixene malate Cat. No.: HY-B0274 Cat. No.: HY-B1613A

Bioactivity: has strong binding affinities to dopamine and Bioactivity: Clebopride malate is a dopamine antagonist drug with histamine receptors, such as D1, D2, D3, D5, H1, 5-HT2, 5-HT6 antiemetic and prokinetic properties used to treat functional and 5-HT7, with Ki of 18 nM, 2.96 nM, 4.56 nM, 9 nM, 3.75 nM, gastrointestinal disorders. 9.4 nM, 3 nM and 5.6 nM, respectively.

Purity: 99.52% Purity: 99.46% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 200 mg, 500 mg 5 mg, 10 mg, 50 mg, 100 mg

Clocapramine Clocapramine hydrochloride hydrate (Clocarpramine; 3-Chlorocarpipramine) Cat. No.: HY-B2073 (3-Chlorocarpipramine hydrochloride hydrate) Cat. No.: HY-B2073A

Bioactivity: Clocapramine is an antagonist of the D2, 5-HT2A Bioactivity: Clocapramine hydrochloride hydrate is an antagonist of the D and 5-HT receptors. receptors. 2 2A

Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 1 mg Size: 1 mg

www.MedChemExpress.com 55

Clomipramine hydrochloride Clozapine Cat. No.: HY-B0457 (HF 1854) Cat. No.: HY-14539

Bioactivity: HCl is a serotonin transporter (SERT), Bioactivity: Clozapine (HF 1854) is an antipsychotic used to treat norepinephrine transporter (NET) dopamine transporter (DAT) schizophrenia. Clozapine is a potent antagonist of dopamine

blocker with Ki of 0.14, 54 and 3 nM, respectively. Target: and a number of other receptors, with a Ki of 9.5 nM for M1 5-HT Receptor Clomipramine hydrochloride (Anafranil) is a receptor. hydrochloride salt of clomipramine which is a serotonin… Purity: 99.72% Purity: 99.97% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 100 mg, 500 mg, 5 g

Dexpramipexole Dexpramipexole dihydrochloride ((R)- ((R)-Pramipexole; R-(+)-Pramipexole; KNS-760704) Cat. No.: HY-17355B (dihydrochloride); …) Cat. No.: HY-17355A

Bioactivity: Dexpramipexole(KNS-760704), also known as R-(+)-Pramipexole, Bioactivity: Dexpramipexole dihydrochloride, also known as is a neuroprotective agent and weak non-ergoline dopamine R-(+)-Pramipexole, is a neuroprotective agent and weak agonist. IC50 Value: non-ergoline . IC50 Value: Target: Dopamine Receptor Dexpramipexole has been found to have neuroprotective effects and is being investigated for treatment of amyotrophic… Purity: >98% Purity: 98.01% Clinical Data: Phase 3 Clinical Data: Phase 3 Size: 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

Dicarbine Cat. No.: HY-127086 (R33812) Cat. No.: HY-B0411

Bioactivity: Dicarbine blocks dopamine receptors in various brain parts Bioactivity: Domperidone is a dopamine blocker and an antidopaminergic and prevents the depression of the conditioned defence reagent. reflexes caused by stimulation of the mesencephalic portion of the reticular formation. Dicarbine could be used to treat patients with schizophrenia and alcoholic psychosis in… Purity: >98% Purity: 99.52% Clinical Data: No Development Reported Clinical Data: Launched Size: Size: 10mM x 1mL in DMSO, 100 mg, 200 mg, 500 mg

Dopamine hydrochloride Dopamine serotonin antagonist-1 (ASL279) Cat. No.: HY-B0451A Cat. No.: HY-42110

Bioactivity: Dopamine HCl is a catecholamine neurotransmitter present in a Bioactivity: Dopamine serotonin antagonist-1 is a dual dopamine and wide variety of animals,And a dopamine D1-5 receptors agonist. serotonin receptor antagonist with Kis of 200, 2500, 420, 39, Target: Dopamine Receptor Dopamine (or 84, 40 nM for dopamine D1, D2,D4, and serotonin S2A, S2C, S3, 3,4-dihydroxyphenethylamine) is a neuroendocrine transmitter respectively. in the catecholamine and families that plays a… Purity: 98.0% Purity: 99.79% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 10 mg, 50 mg, 100 mg

Droperidol (Dehydrobenzperidol) Cat. No.: HY-B1240 (SKF 82526) Cat. No.: HY-B0735

Bioactivity: is a Dopamine-2 Receptor Antagonist. Bioactivity: Fenoldopam(SKF 82526) is a drug and synthetic derivative which acts as a selective D1 receptor partial agonist.

Purity: 99.29% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg 100 mg

56 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Fenoldopam mesylate dihydrochloride (Fenoldopam methanesulfonate; SKF-82526 mesylate) Cat. No.: HY-B0735A Cat. No.: HY-A0081

Bioactivity: Fenoldopam(SKF 82526) mesylate is a drug and synthetic Bioactivity: Fluphenazine dihydrochloride is a -class D1DR and benzazepine derivative which acts as a selective D1 receptor D2DR inhibitor; used to deliver Fluphenazine to biological partial agonist. systems in studies probing the effects and metabolic fates of this commonly used dopamine antagonist.

Purity: 99.85% Purity: 99.96% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg 10 mg, 50 mg, 100 mg

Foscarbidopa Foslevodopa ( 4′-monophosphate) Cat. No.: HY-109131 (Dopa 4-​Phosphate; 3-Hydroxy-O-phosphono-L-tyrosine) Cat. No.: HY-109132

Bioactivity: Foscarbidopa (Carbidopa 4′-monophosphate) is a of Bioactivity: Foslevodopa is a dopamine receptor agonist [1]. Carbidopa, acts as a dopamine receptor agonist [1] [2].

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size:

GSK163090 GSK598809 Cat. No.: HY-14348 Cat. No.: HY-19654

Bioactivity: GSK163090 is a potent, selective, and orally active 5-HT1A/B/D Bioactivity: GSK598809 is a potent and selective dopamine D3 Receptor

receptor antagonist with pKi of 9.4/8.5/9.7, and 6.3/6.7 for (DRD3) antagonist, with a pKi of 8.9. 5-HT1A/B/D, and dopamine D2/D3, respectively.

Purity: 99.95% Purity: 99.73% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Haloperidol D4 Cat. No.: HY-14538 Cat. No.: HY-14538S

Bioactivity: Haloperidol is a potent dopamine D2 receptor antagonist, Bioactivity: Haloperidol D4 is deuterium labeled haloperidol, and the widely used as an antipsychotic. latter is a potent dopamine D2 receptor antagonist.

Purity: 99.72% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg 100 mg, 500 mg

Haloperidol D4' Haloperidol hydrochloride Cat. No.: HY-14538S1 Cat. No.: HY-14538A

Bioactivity: Haloperidol D4' is deuterium labeled haloperidol, and the Bioactivity: Haloperidol hydrochloride is a potent dopamine D2 receptor latter is a potent dopamine D2 receptor antagonist. antagonist, widely used as an antipsychotic.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg Size: 100 mg, 500 mg

www.MedChemExpress.com 57

Iloperidone Iloperidone hydrochloride (HP 873) Cat. No.: HY-17410 (HP 873 hydrochloride) Cat. No.: HY-17410A

Bioactivity: Iloperidone(HP 873) is a D2/5-HT2 receptor antagonist, which Bioactivity: Iloperidone (hydrochloride) is a D(2)/5-HT(2) receptor is an atypical antipsychotic for the treatment of antagonistis, which is an atypical antipsychotic for the schizophrenia symptoms. treatment of schizophrenia symptoms.

Purity: 99.93% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

L-DOPA (Levodopa; 3,4-Dihydroxyphenylalanine) Cat. No.: HY-N0304 (RV-12309; S-(-)-) Cat. No.: HY-B1059

Bioactivity: L-DOPA is a natural form of DOPA used in the treatment of Bioactivity: Levosulpiride (RV-12309) is the (S)-enantiomer of sulpiride, Parkinson's disease. L-DOPA is the precursor of dopamine and which is a D2 receptor a antagonist, an atypical antipsychotic product of . Target: Dopamine Receptor drug of the benzamide class. L-DOPA (L-3,4-dihydroxyphenylalanine) is a chemical that is made and used as part of the normal biology of humans, some… Purity: >98% Purity: 99.99% Clinical Data: Launched Clinical Data: Launched Size: 200 mg, 1 g Size: 10mM x 1mL in DMSO, 100 mg

lumateperone Tosylate Lurasidone (ITI-007) Cat. No.: HY-19733 (SM-13496) Cat. No.: HY-B0032A

Bioactivity: Lumateperone Tosylate is a 5-HT2A receptor antagonist (Ki = Bioactivity: Lurasidone (SM-13496) is an antagonist of both dopamine 0.54 nM), a partial agonist of presynaptic D2 receptors and an D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a respectively. Lurasidone (SM-13496) is also a partial agonist SERT blocker (Ki = 61 nM). IC50 value: 0.54 nM (Ki, for 5-HT2A of 5-HT receptor with an IC of 6.75 nM. receptor ) Target: 5-HT2A receptor Lumateperone also possesses… 1A 50 Purity: 99.21% Purity: 99.33% Clinical Data: Phase 3 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Lurasidone Hydrochloride (SM-13496 (Hydrochloride)) Cat. No.: HY-B0032 Cat. No.: HY-17382

Bioactivity: Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an Bioactivity: Metoclopramide is a dopamine D2 antagonist that is used as an

antagonist of both dopamine D2 and 5-HT7 with IC50s of antiemetic. IC50 Value: Target: D2 Receptor Metoclopramide is 1.68 and 0.495 nM, respectively. Lurasidone (Hydrochloride) a dopamine receptor antagonist which has been used for (SM-13496 (Hydrochloride)) is also a partial agonist… treatment of a variety of gastrointestinal symptoms over the last thirty years. In various countries, metoclopramide is the… Purity: 99.87% Purity: 99.94% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg, 100 mg, 200 mg, 500 mg Size: 10mM x 1mL in DMSO, 100 mg, 500 mg

Metoclopramide hydrochloride hydrate hydrochloride (Metoclopramide monohydrochloride monohydrate) Cat. No.: HY-17382A (EN-1733A) Cat. No.: HY-B1017

Bioactivity: Metoclopramide hydrochloride hydrate is a dopamine D2 Bioactivity: Molindone is a therapeutic antipsychotic, used in the antagonist that is used as an antiemetic. IC50 Value: Target: treatment of schizophrenia, works by blocking the effects of D2 Receptor Metoclopramide is a dopamine receptor antagonist dopamine in the brain, leading to diminished psychoses. which has been used for treatment of a variety of gastrointestinal symptoms over the last thirty years. In… Purity: 99.94% Purity: 99.92% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 10 mg, 50 mg

58 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

NEO 376 Neuromedin N (SPI-376) Cat. No.: HY-101583 (Neuromedin N (rat, mouse, porcine, canine)) Cat. No.: HY-P0079

Bioactivity: NEO 376 is a selective modulator of 5-HT1 receptor, GABA Bioactivity: Neuromedin N is a potent modulator of dopamine D2 receptor receptor and dopamine receptor, with anti-psychotic agonist binding in rat neostriatal membranes. actively.

Purity: >98% Purity: 99.91% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in Water, 5 mg, 10 mg, 25 mg

NMI 8739 Cat. No.: HY-101540 ((±)-Nomifensin) Cat. No.: HY-B1110

Bioactivity: NMI 8739 is a dopamine D2 autoreceptor agonist, which is Bioactivity: Nomifensine is a norepinephrine-dopamine reuptake inhibitor, an amine conjugate of the DHA carrier and the neurotransmitter increases the amount of synaptic norepinephrine and dopamine dopamine. available to receptors by blocking the dopamine and norepinephrine reuptake transporters.

Purity: >98% Purity: 99.24% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg 50 mg, 100 mg

Nomifensine maleate NRA-0160 ((±)-Nomifensine maleat) Cat. No.: HY-B1110A Cat. No.: HY-101641

Bioactivity: Nomifensine maleate is a selective inhibitor of dopamine Bioactivity: NRA-0160 is a selective dopamine D4 receptor antagonist, uptake, used in adult attention deficit disorder. with a Ki value of 0.48 nM and with negligible affinity for

dopamine D2 receptor ( Ki: >10000 nM), D3 receptor (

Ki: 39 nM), rat 5-HT2A receptor ( Ki: 180 nM) and rat Purity: 98.14% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 50 mg, 100 mg

Nuciferine Ocaperidone Cat. No.: HY-N0049 (R79598) Cat. No.: HY-101094

Bioactivity: Nuciferine is an antagonist at 5-HT2A ( IC50=478 nM), Bioactivity: Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT2 and dopamine D2 antagonist, and a 5-HT1A 5-HT2C ( IC50=131 nM), and 5-HT2B ( IC50=1 μM), an inverse agonist, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 agonist at 5-HT7 ( IC50=150 nM), a partial agonist at D2 ( nM for 5-HT 2, a 1-adrenergic receptor, dopamine D 2 EC50=64 nM), D5 ( EC50=2.6 μM) and 5-HT6 ( EC50=… Purity: 99.66% Purity: 98.55% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg 5 mg, 10 mg, 50 mg, 100 mg

Org-10490 hydrobromide Cat. No.: HY-U00077 (6-Hydroxydopamine hydrobromide; 6-OHDA hydrobromide)Cat. No.: HY-B1081A

Bioactivity: Org-10490 is an antagonist of dopamine D1 receptor and Bioactivity: Oxidopamine (hydrobromide), an antagonist of the dopamine D2 receptor, used for the treatment for neurotransmitter dopamine, is a widely used psychiatric disease. that selectively destroys dopaminergic neurons.

Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 200 mg, 500 mg, 1 g

www.MedChemExpress.com 59

Paliperidone Pardoprunox (9-hydroxyrisperidone) Cat. No.: HY-A0019 (SLV-308; DU-126891) Cat. No.: HY-14958

Bioactivity: (9-hydroxyrisperidone is a dopamine antagonist of Bioactivity: Pardoprunox(SLV-308) is a novel partial dopamine D2 and D3 the atypical antipsychotic class of medications. receptor agonist and serotonin 5-HT1A receptor agonist; D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist (IA = 50% and 67%, respectively) and 5-HT1A receptor (pKi = 8.5) full agonist (IA = 100%); also binds to D4 (pKi = 7.8),… Purity: 99.09% Purity: >98% Clinical Data: Launched Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 50 mg, 100 mg, 200 mg, 500 mg

Pardoprunox hydrochloride PD-168077 maleate (SLV-308 hydrochloride; DU-126891 hydrochloride) Cat. No.: HY-14958A Cat. No.: HY-21098A

Bioactivity: Pardoprunox hydrochloride is a novel partial dopamine D2 and Bioactivity: PD-168077 maleate is a selective dopamine D4 receptor D3 receptor agonist and serotonin 5-HT1A receptor agonist, D2 agonist, with a K of 9 nM. (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist and i 5-HT1A receptor (pKi = 8.5) full agonist.

Purity: 98.89% Purity: 98.44% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Pentiapine mesylate (CGS 10746) Cat. No.: HY-100143 (Pergolide methanesulfonate; LY127809) Cat. No.: HY-13720A

Bioactivity: Pentiapine is a novel dopamine release inhibitor. Bioactivity: Pergolide Mesylate is an antiparkinsonian agent which functions as a dopaminergic agonist. Target: Dopamine Receptor Pergolide mesylate (trade name Permax) is an ergoline-based dopamine receptor agonist used in some countries for the treatment of Parkinson's disease. Pergolide mesylate functions… Purity: >98% Purity: 99.93% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg

Perphenazine Perphenazine D8 Dihydrochloride Cat. No.: HY-A0077 Cat. No.: HY-A0077AS

Bioactivity: Perphenazine is a typical antipsychotic drug, inhibits Bioactivity: Perphenazine D8 Dihydrochloride is the deuterium labeled

5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine Perphenazine, which is a typical antipsychotic drug(5-HT, receptor D2/D3, D2L receptor, and Histamine H1 receptor, Dopamine receptor ligand).

with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 … Purity: 99.90% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 1 g, 5 g

PF-592379 Pimethixene Cat. No.: HY-U00400 (Pimetixene) Cat. No.: HY-B1101

Bioactivity: PF-592379 is a potent dopamine D3 receptor agonist with Bioactivity: Pimethixene is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene is a highly potent an EC50 of 21 nM. antagonist of 5-HT 1A, 5-HT 2A, 5-HT 2B, 5-HT 2C,

histamine H 1, dopamine D 2 and D 4.4 as well as muscari… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10 mg

60 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Pimethixene maleate (Pimetixene maleate) Cat. No.: HY-B1101A (R6238) Cat. No.: HY-12987

Bioactivity: Pimethixene maleate is antihistamine and antiserotonergic Bioactivity: Pimozide is a dopamine receptor antagonist, with Kis of compound, acts as an antimigraine agent. Pimethixene maleate 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 is a highly potent antagonist of 5-HT 1A, 5-HT 2A, 5-HT 2B, receptors, respectively, and also has affinity at 5-HT , histamine H , dopamine D and D as well… 2C 1 2 4.4 α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhib… Purity: >98% Purity: 99.88% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mg Size: 10mM x 1mL in DMSO, 50 mg

Piperidine-MO-1 Cat. No.: HY-19845A Cat. No.: HY-12707

Bioactivity: -MO-1 is a modulator of dopamine receptor Bioactivity: Piribedil is a dopamine D2 receptor ( D2R) agonist extracted from patent WO/2005/121087A1, compound example 2; which also displays antagonist property at hα -adrenoceptor exhibits an ED of 68 μmol/kg on increase of DOPAC in the 1A 50 ( hα -AR). rat striatum. 1A

Purity: >98% Purity: 99.90% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

Piribedil D8 Pramipexole (ET-495 D8) Cat. No.: HY-12707S Cat. No.: HY-B0410

Bioactivity: Piribedil D8 is the deuterium labeled Piribedil, which is an Bioactivity: Pramipexole is a dopamine agonist of the non-ergoline class antiparkinsonian agent. indicated for treating Parkinson's disease (PD) and (RLS).

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg Size: 50 mg, 100 mg

Pramipexole dihydrochloride Cat. No.: HY-17355 (ACR16; ASP2314; FR310826) Cat. No.: HY-10684

Bioactivity: Pramipexole 2Hcl is a partial/full D2S, D2L, D3, D4 receptor Bioactivity: Pridopidine, a dopamine ( DA) stabilizer, acts as a low agonist with a Ki of 3.9, 2.2, 0.5 and 5.1 nM for D2S, D2L, affinity dopamine D2 receptor ( D2R) antagonist. D3, D4 receptor, respectively. IC50 Value: 3.9 nM(D2S); 2.2 Pridopidine exerts high affinity towards sigma 1 receptor nM(D2L); 0.5 nM(D3); 5.1 nM(D4) Target: Dopamine Receptor ( S1R) with Ki between 70 and 80 nM, which is ~100× higher Pramipexole dihydrochloride is a dopamine receptor agonist… than its affinity toward D2R. Purity: 98.0% Purity: 99.76% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Prochlorperazine D8 D8 dimeleate Cat. No.: HY-B0807S Cat. No.: HY-B0807S1

Bioactivity: Prochlorperazine D8 is the deuterium labeled Prochlorperazine, Bioactivity: Prochlorperazine D8 dimeleate is the deuterium labeled which is a dopamine (D2) receptor antagonist. Prochlorperazine, which is a dopamine (D2) receptor antagonist.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg

www.MedChemExpress.com 61

Promazine hydrochloride Quetiapine D4 fumarate Cat. No.: HY-B1225 Cat. No.: HY-B0031S

Bioactivity: (hydrochloride) is a D2 dopamine receptor Bioactivity: Quetiapine D4 fumarate is the deuterium labeled Quetiapine, antagonist, belongs to the phenothiazine class of which is an atypical antipsychotic. antipsychotics, used to treat schizophrenia.

Purity: 99.72% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 1 mg, 5 mg, 10 mg 100 mg

Quetiapine fumarate hydrochloride Cat. No.: HY-B0031 (CV205-502 hydrochloride) Cat. No.: HY-13736A

Bioactivity: Quetiapine fumarate is an atypical antipsychotic used in the Bioactivity: Quinagolide hydrochloride is a selective dopamine D2 receptor treatment of schizophrenia, bipolar I mania, bipolar II agonist, also is a inhibitor. Target: dopamine D2 depression, bipolar I depression. receptor, prolactin Quinagolide is a selective, D2 receptor agonist (or prolactin-release inhibitor) that is used for the treatment of elevated levels of prolactin. Quinagolide is… Purity: 99.54 Purity: 99.96% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 5 mg, 10 mg, 50 mg, 100 mg

Quinpirole Hydrochloride rac-Rotigotine Hydrochloride ((-)-LY 171555) Cat. No.: HY-B1752A Cat. No.: HY-15394

Bioactivity: (Hydrochloride) is a high-affinity agonist Bioactivity: rac-Rotigotine Hcl is a high potency and selectivity agonist dopamine D2/D3 receptor. for D-2 receptor with Ki of 0.69 nM.

Purity: >98% Purity: 97.76% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg

Raclopride Risperidone Cat. No.: HY-103414 (R 64 766) Cat. No.: HY-11018

Bioactivity: is a dopamine D2/ D3 receptor antagonist, Bioactivity: Risperidone is a serotonin 5-HT2 receptor blocker,

which binds to D2 and D3 receptors with dissociation P-Glycoprotein inhibitor and potent dopamine D2 receptor

constants ( Kis) of 1.8 nM and 3.5 nM, respectively, but has a antagonist, with Kis of 4.8, 5.9 nM for 5-HT 2A and dopamine

very low affinity for D 1 and D 4 receptors with K is… D 2 receptor, respectively. Purity: >98% Purity: 99.16% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg 10 mg, 50 mg, 100 mg

Risperidone hydrochloride Risperidone mesylate (R 64 766 hydrochloride) Cat. No.: HY-11018A (R 64 766 mesylate) Cat. No.: HY-11018B

Bioactivity: Risperidone hydrochloride is a serotonin 5-HT2 receptor Bioactivity: Risperidone mesylate(R 64 766 mesylate) is a serotonin 5-HT2 blocker and a potent dopamine D receptor antagonist, receptor blocker(Ki= 0.16 nM) and a potent dopamine D2 2 receptor antagonist(Ki= 1.4 nM). with Kis of 0.16, 1.4 nM for 5-HT 2 and D 2 receptor, respectively. Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg, 100 mg Size: 10 mg, 50 mg, 100 mg

62 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Ro 10-5824 dihydrochloride hydrochloride Cat. No.: HY-101384A (SKF 101468 hydrochloride) Cat. No.: HY-B0623A

Bioactivity: Ro 10-5824 dihydrochloride is a selective dopamine D4 Bioactivity: Ropinirole hydrochloride(SKF101468 hydrochloride) a selective dopamine D2 receptor inhibitor with IC50 of 29 nM. receptor partial agonist, with Ki of 5.2 nM.

Purity: 98.89% Purity: 99.93% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 50 mg, 100 mg, 200 mg

Rotigotine Rotigotine D7 Hydrochloride (N-0437; N-0923) Cat. No.: HY-75502 (N-0923 D7 Hydrochloride) Cat. No.: HY-A0007S

Bioactivity: Rotigotine is a full agonist of dopamine receptor, a Bioactivity: Rotigotine D7 Hydrochloride is the deuterium labeled partial agonist of the 5-HT1A receptor, and an antagonist of Rotigotine(N-0923), which is a dopamine D2 and D3 receptor agonist. the α2B-adrenergic receptor, with Kis of 0.71nM, 4-15nM, and 83nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor. Purity: 99.98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 10 mg, 50 mg, 100 mg

Rotundine SB-277011 ((-)-Tetrahydropalmatine; L-Tetrahydropalmatine) Cat. No.: HY-N0096 (SB-277011A) Cat. No.: HY-10847

Bioactivity: Rotundine is an antagonist of dopamine D1, D2 and D3 Bioactivity: SB-277011 is a potent and delective dopamine D3 receptor antagonist (pKi values are 8.0, 6.0, 5.0 and <5.2 for D3, receptors with IC50s of 166 nM, 1.4 μM and 3.3 μM, D2, 5-HT1D and 5-HT1B respectively); brain penetrant. respectively. Rotundine is also an antagonist of 5-HT1A with

an IC50 of 370 nM. Purity: 99.88% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 50 mg

SB-277011 dihydrochloride SB269652 (SB-277011A dihydrochloride) Cat. No.: HY-10847A Cat. No.: HY-12324

Bioactivity: SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a Bioactivity: SB269652 is the first drug-like of the potent, selective, orally bioavailable and brain penetrate dopamine D2 receptor (D2R); a new chemical probe that can

dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, differentiate D2R monomers from dimers or oligomers depending on the observed pharmacology. <5.2 and 5.9 for D 3, D 2, 5-HT 1B, and 5-HT 1D Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 5 mg, 10 mg, 50 mg, 100 mg

SCH 23390 hydrochloride Sertindole (R-(+)-SCH23390 hydrochloride) Cat. No.: HY-19545A (Lu 23-174) Cat. No.: HY-14543

Bioactivity: SCH 23390 hydrochloride is a potent Bioactivity: Sertindole, a neuroleptic, is one of the newer antipsychotic

antagonist with Ki values of 0.2 and 0.3 nM for the D1 and D5. medications available. Target: Multi-target In vitro studies showed that sertindole exerts a potent antagonism at serotonin 5-HT2A, 5-HT2C, dopamine D2, and αl adrenergic receptors. Sertindole offers an alternative treatment option for… Purity: 99.31% Purity: 96.14% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 10 mg, 50 mg

www.MedChemExpress.com 63

SKF 38393 hydrochloride SKF 82958 ((±)-SKF-38393 hydrochloride; SKF-38393A) Cat. No.: HY-12520A ((±)-SKF 82958; Chloro-AP) Cat. No.: HY-10435

Bioactivity: SKF 38393 hydrochloride is a selective agonist of the Bioactivity: SKF 82958 is a D1/D5 receptor full agonist. IC50 value: [1] Target: D1/D5 receptor in vitro: Neuropeptide and immediate dopamine D1 receptor (D1DR) with an IC50 of 110 nM . early gene expression in striatonigral neurons of the normosensitive striatum is induced by mixed D1 receptor SKF-82958, which induces behavioral activity and… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 50 mg, 100 mg, 200 mg, 500 mg Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

SKF-82958 hydrobromide ST-836 ((±)-SKF 82958 hydrobromide; Chloro-APB hydrobromide) Cat. No.: HY-10435A Cat. No.: HY-15238

Bioactivity: SKF-82958 hydrobromide is a D1/D5 receptor full agonist. IC50 Bioactivity: ST-836 is a dopamine receptor ligand; Antiparkinsonian agent. value: Target: D1/D5 receptor in vitro: Neuropeptide and immediate early gene expression in striatonigral neurons of the normosensitive striatum is induced by mixed D1 receptor SKF-82958, which induces behavioral activity and… Purity: 99.95% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

ST-836 hydrochloride Sulpiride Cat. No.: HY-15238A Cat. No.: HY-B1019

Bioactivity: ST-836 Hcl is a dopamine receptor ligand; Antiparkinsonian Bioactivity: Sulpiride is a D2 receptor a antagonist, an atypical agent. antipsychotic drug of the benzamide class, used mainly in the treatment of psychosis associated with schizophrenia and major depressive disorder, and sometimes used in low dosage to treat anxiety and mild depression. Purity: 98.01% Purity: 99.99% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 100 mg

Sultopride hydrochloride (LIN-1418) Cat. No.: HY-42849 (LIN-1418 hydrochloride) Cat. No.: HY-42849A

Bioactivity: Sultopride is a selective antagonist of dopamine D2 Bioactivity: Sultopride hydrochloride is a selective antagonist of receptor. dopamine D2 receptor.

Purity: >98% Purity: 99.96% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 25 mg, 50 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg

Sumanirole maleate Talipexole (U-95666E; PNU-95666) Cat. No.: HY-70081A (B-HT 920) Cat. No.: HY-A0040

Bioactivity: maleate(PNU 95666E; U95666E) is a highly selective Bioactivity: Talipexole (B-HT920) is a dopamine agonist that has been D2 receptor full agonist with an ED50 of about 46 nM. IC50 proposed as an antiparkinsonian agent. Target: Dopamine value: 46 nM (EC50) Target: D2 receptor Sumanirole was Receptor B-HT920 is a selective alpha 2-adrenoceptor agonist. developed for the treatment of Parkinson's disease and The effects of B-HT920 have been specified using the restless leg syndrome. While it has never been approved for… alpha-adrenergic antagonists and and the… Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 25 mg, 50 mg, 100 mg

64 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Talipexole dihydrochloride Tetrahydroberberine (B-HT 920 (dihydrochloride)) Cat. No.: HY-A0008 () Cat. No.: HY-N0925

Bioactivity: Talipexole dihydrochloride (B-HT 920 dihydrochloride) is a Bioactivity: Tetrahydroberberine is an isoquinoline alkaloid isolated from dopamine D2 receptor agonist, α2-adrenoceptor agonist and corydalis tuber; has micromolar affinity for dopamine D(2) 5-HT3 receptor antagonist, which displays antiParkinsonian (pK(i) = 6.08) and 5-HT(1A) (pK(i) = 5.38) receptors but activity. moderate to no affinity for other relevant serotonin receptors (5-HT(1B), 5-HT(1D), 5-HT(3), and 5-HT(4); pK(i) < 5.00). Purity: 99.99% Purity: 99.70% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 5 mg, 10 mg

Tetrahydropalmatine Thioridazine hydrochloride (DL-Tetrahydropalmatine) Cat. No.: HY-N0300 Cat. No.: HY-B0965

Bioactivity: Tetrahydropalmatine, an active component isolated from Bioactivity: Thioridazine is an antipsychotic drug, used in the treatment corydalis, acts through inhibition of amygdaloid release of of schizophrenia and psychosis, shows D4 selectivity or dopamine to inhibit an epileptic attack in rats. serotonin antagonism.

Purity: 99.07% Purity: 99.93% Clinical Data: No Development Reported Clinical Data: Phase 4 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 100 mg, 500 mg

Tiapride hydrochloride dihydrochloride Cat. No.: HY-B1196 (TFP; SKF5019) Cat. No.: HY-B0532A

Bioactivity: hydrochloride is a drug that selectively blocks D2 Bioactivity: Trifluoperazine Dihydrochloride is a potent dopamine D2 and D3 dopamine receptors in the brain. It is used to treat a receptor inhibitor used as an antipsychotic and an antiemetic. variety of neurological and psychiatric disorders including Target: Dopamine D2 Receptor Trifluoperazine Dihydrochloride , withdrawal syndrome. is a potent dopamine D2 receptor inhibitor used as an antipsychotic and an antiemetic. Trifluoperazine inhibited in… Purity: 99.82% Purity: 99.0% Clinical Data: Launched Clinical Data: Launched Size: 100 mg Size: 10mM x 1mL in DMSO, 100 mg, 500 mg

Triflupromazine hydrochloride hydrochloride Cat. No.: HY-B0909 (Ro 2-9578) Cat. No.: HY-12751A

Bioactivity: hydrochloride is an antipsychotic , Bioactivity: Trimethobenzamide hydrochloride is a blocker of the D2 which are Dopamine D1/D2 receptor antagonists. receptor. Trimethobenzamide is an antiemetic used to prevent nausea and vomiting.

Purity: 99.94% Purity: 99.70% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 100 mg, 200 mg, 500 mg

U91356 Cat. No.: HY-U00227 ((±)-Veralipride; LIR166) Cat. No.: HY-101797

Bioactivity: U91356 is a dopamine receptor agonist. Bioactivity: Veralipride is a D2 receptor antagonist. It is an alternative antidopaminergic treatment for menopausal symptoms.

Purity: >98% Purity: 99.12% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 65

Ziprasidone Ziprasidone D8 (CP-88059) Cat. No.: HY-14542 (CP-88059 D8) Cat. No.: HY-14542S

Bioactivity: Ziprasidone(CP88059) is a combined 5-HT (serotonin) and Bioactivity: Ziprasidone D8 is deuterium labeled Ziprasidone, which is a dopamine receptor antagonist which exhibits potent effects of combined 5-HT (serotonin) and dopamine receptor antagonist antipsychotic activity. which exhibits potent effects of antipsychotic activity.

Purity: 98.69% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg 10 mg, 50 mg

Ziprasidone hydrochloride Ziprasidone hydrochloride monohydrate (CP-88059 hydrochloride) Cat. No.: HY-14542A (CP 88059 (hydrochloride monohydrate)) Cat. No.: HY-17407

Bioactivity: Ziprasidone Hcl(CP-88059 Hcl) is a combined 5-HT (serotonin) Bioactivity: Ziprasidone hydrochloride monohydrate (CP 88059 hydrochloride and dopamine receptor antagonist which exhibits potent effects monohydrate) is a combined 5-HT (serotonin) and dopamine of antipsychotic activity. receptor antagonist which exhibits potent effects of antipsychotic activity. Target: 5-HT receptor; Dopamine receptor Ziprasidone hydrochloride monohydrate is the salt… Purity: >98% Purity: 99.83% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

Zuclopenthixol ((Z)-) Cat. No.: HY-A0163

Bioactivity: is a derivative which acts as a mixed dopamine D1/D2 receptor antagonist.

Purity: 98.80% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 50 mg

66 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Dopamine Transporter DAT;SLC6A3

Dopamine Transporter (DAT) is an integral membrane protein that removes dopamine from the synaptic cleft and deposits it into surrounding cells, thus terminating the signal of the neurotransmitter. Dopamine transporter (DAT) controls the spatial and temporal dynamics of dopamine (DA) neurotransmission by driving reuptake of extracellular transmitter into presynaptic neurons. Many diseases such as depression, , Parkinson’s disease, and attention deficit hyperactivity disorder are associated with abnormal DA levels, implicating DAT as a factor in their etiology. Medications used to treat these disorders and many addictive drugs target DAT and enhance dopaminergic signaling by suppressing transmitter reuptake. DAT is regulated by multiple signaling systems, with PKC and ERK being two of the most well-characterized.

www.MedChemExpress.com 67 Dopamine Transporter Inhibitors & Modulators

Amitifadine hydrochloride (DOV-21947 hydrochloride; EB-1010 hydrochloride) Cat. No.: HY-18332A (EB-1020) Cat. No.: HY-16736

Bioactivity: hydrochloride is a Bioactivity: Centanafadine is dual norepinephrine (NE)/dopamine (DA) serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI), transporter inhibitor, also inhibits serotonin transporter,

with IC50s of 12, 23, 96 nM for serotonin, norepinephrine and with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and dopamine in HEK 293 cells , respectively. serotonin transporter , respectively.

Purity: 99.92% Purity: >98% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 5 mg, 10 mg, 50 mg

Centanafadine hydrochloride (EB-1020 (hydrochloride)) Cat. No.: HY-16736A (SEP 225289) Cat. No.: HY-12850

Bioactivity: Centanafadine (hydrochloride) is dual norepinephrine Bioactivity: Dasotraline is a triple reuptake inhibitor that blocks (NE)/dopamine (DA) transporter inhibitor, also inhibits dopamine, norepinephrine, and serotonin transporters with IC values of 4, 6, and 11 nM, respectively. serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for 50 human NE, DA and serotonin transporter , respectively.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

Dasotraline hydrochloride Desipramine hydrochloride (SEP-225289 hydrochloride) Cat. No.: HY-12850A Cat. No.: HY-B1272

Bioactivity: Dasotraline hydrochloride (SEP-225289 hydrochloride) is a Bioactivity: Desipramine hydrochloride is an inhibitor of norepinephrine triple reuptake inhibitor that blocks dopamine, transporter ( NET), 5-HT transporter ( SERT) and norepinephrine, and serotonin transporters with IC values of 50 dopamine transporter ( DAT) with Kis of 4, 61 and 78,720 4, 6, and 11 nM, respectively. nM, respectively.

Purity: 99.60% Purity: 99.68% Clinical Data: Phase 3 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg 100 mg, 500 mg

Diclofensine hydrochloride (Ro 8-4650) Cat. No.: HY-18610A (Ro 8-4650 hydrochloride) Cat. No.: HY-18610

Bioactivity: Diclofensine(Ro-8-4650) is a potent inhibitor of monoamine Bioactivity: Diclofensine(Ro-8-4650) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively. 2.3, and 3.7 nM, respectively.

Purity: >98% Purity: 96.44% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg Size: 10mM x 1mL in Water, 5 mg, 10 mg, 50 mg

DOV-216,303 Free Base Cat. No.: HY-18332C Cat. No.: HY-B1124

Bioactivity: DOV-216,303 (Free Base) is a potent triple serotonin, Bioactivity: Fipexide is a psychoactive drug of the chemical

norepinephrine, and dopamine reuptake inhibitor, with IC50 class, used as a drug, mainly for the treatment of values of 14 nM, 20 nM and 78 nM for hSERT, hNET and hDAT, senile dementia. respectively [1]. Has antidepressant-like effects … Purity: 98.47% Purity: 99.87% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg 100 mg

68 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

GBR 12935 GBR 12935 dihydrochloride Cat. No.: HY-12242A Cat. No.: HY-12242

Bioactivity: GBR 12935 is a potent, and selective dopamine reuptake Bioactivity: GBR 12935 dihydrochloride is a potent, and selective dopamine inhibitor. IC50 value: Target: dopamine reuptake inhibitor in reuptake inhibitor. IC50 value: Target: dopamine reuptake vitro: The calculated Kd of [3H]GBR-12935 binding to CYP2D6 inhibitor in vitro: The calculated Kd of [3H]GBR-12935 binding was 42.2 nM, indicating that GBR-12935 has a high affinity for to CYP2D6 was 42.2 nM, indicating that GBR-12935 has a high CYP2D6. The binding of [3H]GBR-12935 to CYP2D6 was decreased… affinity for CYP2D6. The binding of [3H]GBR-12935 to CYP2D6… Purity: >98% Purity: 98.90% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg

Levophacetoperane hydrochloride SPD-473 citrate Cat. No.: HY-101631 Cat. No.: HY-101612

Bioactivity: inhibits in vitro in a competitive manner, Bioactivity: SPD-473 citrate is a serotonin/ dopamine/ norepinephrine norepinephrin uptake and dopamine uptake. reuptake inhibitior.

Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 1 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

Vanoxerine dihydrochloride (GBR 12909; I893) Cat. No.: HY-13217A (GBR-12909 dihydrochloride; I893 dihydrochloride) Cat. No.: HY-13217

Bioactivity: Vanoxerine (GBR12909) is a potent and selective DRI (Dopamine Bioactivity: Vanoxerine dihydrochloride is a potent and selective reuptake inhibitor). dopamine reuptake inhibitor.

Purity: >98% Purity: 99.52% Clinical Data: Phase 3 Clinical Data: Phase 3 Size: 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

www.MedChemExpress.com 69 FAAH amide hydrolase

FAAH (Fatty acid amide hydrolase) is an integral membrane enzyme that degrades the fatty acid amide family of signaling lipids, including the endocannabinoid . Genetic or pharmacological inactivation of FAAH leads to analgesic, anti-inflammatory, anxiolytic, and antidepressant phenotypes in rodents without showing the undesirable side effects observed with direct agonists, indicating that FAAH may represent an attractive therapeutic target for treatment of pain, inflammation, and other central nervous system disorders.

70 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] FAAH Inhibitors & Modulators

11C-MK-3168 BIA 10-2474 Cat. No.: HY-111394 Cat. No.: HY-19740

Bioactivity: 11C-MK-3168 is a potent, reversible and blood/brain barrier Bioactivity: BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (

penetrated fatty acid amide hydrolase ( FAAH) inhibitor, with FAAH) with IC50 values of 50 to 70mg/kg in various rat brain IC s of 1.0, 1.7 and 5.5 nM for human, rat and rhesus FAAH, 50 regions. respectively.

Purity: >98% Purity: 98.82% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Biochanin A (4-Methylgenistein; Olmelin) Cat. No.: HY-14595 Cat. No.: HY-B1227

Bioactivity: is a naturally occurring fatty acid amide Bioactivity: Carprofen is a nonsteroid anti-inflammatory agent, acts as a

hydrolase ( FAAH) inhibitor, which inhibits FAAH with IC50s multi-target FAAH/COX inhibitor, with IC50s of 3.9 μM, 22.3 of 1.8, 1.4 and 2.4 μM for mouse, rat, and human FAAH, μM and 78.6 μM for COX-2, COX-1 and FAAH, respectively. respectively.

Purity: 98.86% Purity: 99.76% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 200 mg, 500 mg 100 mg

FAAH inhibitor 1 FAAH-IN-1 Cat. No.: HY-10862 Cat. No.: HY-111389

Bioactivity: FAAH inhibitor 1 is a potent fatty acid amide hydrolase (FAAH) Bioactivity: FAAH-IN-1 is a fatty acid amide hydrolase ( FAAH) inhibitor, inhibitor with an IC50 of 18±8 nM. with IC50s of 145 nM and 650 nM for rat and human FAAH, respectively.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 250 mg, 500 mg

FAAH-IN-2 JNJ-42165279 Cat. No.: HY-79511 Cat. No.: HY-19636

Bioactivity: FAAH-IN-2 is a potent FAAH(fatty acid amide hydrolase) Bioactivity: JNJ-42165279 is a FAAH inhibitor with IC50 of 70 ± 8 nM and inhibitor extracted from Patent WO/2008/100977A2. 313 ± 28 nM for hFAAH and rFAAH, respectively.

Purity: 96.16% Purity: 99.97% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 5 mg, 10 mg, 50 mg, 100 mg

JZL195 LY2183240 Cat. No.: HY-15250 Cat. No.: HY-10865

Bioactivity: JZL195 is a selective and efficacious dual FAAH/MAGL inhibitor Bioactivity: LY2183240 is a novel and highly potent blocker of anandamide with IC50 of 13 nM and 19 nM for mouse brain FAAH and MAGL uptake (IC50 = 270 pM). LY2183240 inhibits fatty acid amide respectively. hydrolase (FAAH) activity (IC50 = 12.4 nM). IC50: 270 pM (anandamide uptake); 12.4 nM (FAAH) Target: FAAH; Anandamide uptake Following i.p. administration in rats, LY2183240… Purity: 99.75% Purity: 99.07% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 10 mg, 50 mg

www.MedChemExpress.com 71

N-Benzylpalmitamide PF 750 (N-Benzylhexadecanamide; Macamide 1) Cat. No.: HY-N2365 Cat. No.: HY-18081

Bioactivity: N-Benzylpalmitamide is a macamide isolated from Lepidium Bioactivity: PF 750 is a selective and covalent fatty acid amide hydrolase meyenii, acts as an inhibitor of fatty acid amide (FAAH) inhibitor, with IC50s varied from 16.2-595 nM in hydrolase (FAAH). different pre-incubation times. Covalently modifies the enzyme’s active site serine nucleophile [1]. Purity: 98.0% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg Size: 5 mg

PF-04457845 PF-3845 Cat. No.: HY-14376 Cat. No.: HY-14380

Bioactivity: PF-04457845 is a highly efficacious and selective FAAH Bioactivity: PF-3845 is a selective fatty acid amide hydrolase (FAAH) inhibitor (Ki = 0.23 μM); showing negligible activity against inhibitor with IC50 values is 7.2±0.63 nM and 7.4±0.62 nM for hFAAH and rFAAH, respectively. FAAH2.

Purity: 99.09% Purity: 98.94% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

SA 47 SA72 Cat. No.: HY-18080 Cat. No.: HY-U00240

Bioactivity: SA 47 is a selective and potent inhibitor of fatty acid amide Bioactivity: SA72 is a highly selective fatty acid amide hydrolase (FAAH) hydrolase (FAAH) and carbamate [1]. inhibitor.

Purity: 99.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg

URB-597 (KDS-4103) Cat. No.: HY-10864

Bioactivity: URB597 is a potent, orally bioavailable FAAH inhibitor with IC50 of 4.6 nM, with no activity on other cannabinoid-related targets. IC50 value: 4.6 nM [1] Target: FAAH in vitro: URB597 binds in the hydrophobic pocket and catalytic core of FAAH that connects the active site residues to the membrane surface… Purity: 98.71% Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg

72 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] GABA Receptor Gamma-aminobutyric acid Receptor;γ-Aminobutyric acid Receptor

GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system. There are two classes of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors), whereas GABAB receptors are G protein-coupled receptors (also known asmetabotropic receptors). It has long been recognized that the fast response of neurons to GABA that is blocked by and is due to direct activation of an anion channel. This channel was subsequently termed the GABAA receptor. Fast-responding GABA receptors are members of family of Cys-loop ligand-gated ion channels. A slow response to GABA is mediated by GABAB receptors, originally defined on the basis of pharmacological properties.

www.MedChemExpress.com 73 GABA Receptor Inhibitors & Modulators

(+)-Bicuculline (+)- (d-Bicuculline) Cat. No.: HY-N0219 (d-Borneol) Cat. No.: HY-N1368A

Bioactivity: (+)-Bicuculline is a light-sensitive competitive antagonist of Bioactivity: (+)-Borneol (d-Borneol) is a natural bicyclic monoterpene used GABA-A receptor. for analgesia and anesthesia in traditional Chinese medicine;

enhances GABA receptor activity with an EC50 of 248 μM.

Purity: 99.97% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 250 mg 100 mg

(+)- (-)-Borneol Cat. No.: HY-B1671 (L-Borneol) Cat. No.: HY-N1368B

Bioactivity: (+)-Kavain, a main extracted from Piper Bioactivity: (-)-Borneol has a highly efficacious positive modulating

methysticum, has anticonvulsive properties, attenuating action at GABA receptor with an EC50 of 237 μM. vascular smooth muscle contraction through interactions with voltage-dependent Na + and Ca 2+ channels [1]. (+)-Kav…

Purity: 99.98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 100 mg

(-)- (R)- Cat. No.: HY-N2079 (STX209) Cat. No.: HY-17354

Bioactivity: (-)-Securinine is plant-derived alkaloid and also a GABAA Bioactivity: (R)-Baclofen(STX209) is a selective GABAB receptor agonist. receptor antagonist. IC50 value: Target: GABAB receptor GABAB receptors are metabotropic receptors which produce slow inhibitory signals. By manipulating GABAB receptor activity using Baclofen, a variety of functions are studied including synaptic… Purity: 98.0% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 5 mg, 10 mg, 25 mg Size: 10mM x 1mL in Water, 10 mg, 50 mg

(R)-Baclofen hydrochloride (S)-SNAP5114 (STX 209 hydrochloride) Cat. No.: HY-17354A Cat. No.: HY-103504

Bioactivity: (R)-Baclofen Hcl(STX-209 Hcl) is a derivative of Bioactivity: (S)-SNAP5114 is a selective GABA transport inhibitor, with gamma-aminobutyric acid (GABA) primarily used to treat IC50 values of 5 μM and 21 μM for hGAT-3 and rGAT-2, spasticity and is in the early research stages for use for the respectively. (S)-SNAP5114 is an anticonvulsant drug [1] treatment of alcoholism. Target: GABA Baclofen (brand names [2] Kemstro, Lioresal, Liofen, Gablofen, Beklo and Baclosan) is a… . Purity: >98% Purity: 98.0% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 5 mg

3,4,5-Trimethoxycinnamic acid 4-Acetamidobutanoic acid Cat. No.: HY-W012123 (N-acetyl GABA) Cat. No.: HY-101411

Bioactivity: 3,4,5-Trimethoxycinnamic acid is a phenylpropanoid isolated Bioactivity: 4-Acetamidobutanoic acid (N-acetyl GABA) is a γ-aminobutyric from the roots of Polygala tenuifolia WILLD, with anti-stress acid ( GABA) derivative. effect, prolonging the sleeping time in animals [1] [2]. 3,4,5-Trimethoxycinnamic acid increases expression of GAD65 and γ-subunit of GABAA receptor, but shows no effect on the… Purity: 99.22% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 100 mg 200 mg

74 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

6,2'-Dihydroxyflavone 6-Methylflavone Cat. No.: HY-N6628 Cat. No.: HY-N6630

Bioactivity: 6,2'-Dihydroxyflavone is a novel antagonist of GABAA Bioactivity: 6-methylflavone is an activator of α 1β 2γ 2L and α 1β 2

receptor. GABAA receptors.

Purity: 99.10% Purity: 99.85% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg 100 mg

Acamprosate calcium (Calcium N-acetylhomotaurinate) Cat. No.: HY-17030 Cat. No.: HY-B1833

Bioactivity: calcium(Campral EC) is a GABA receptor agonist and Bioactivity: Afloqualone is a agonist of GABA receptor . modulator of systems; reduces alcohol consumption in animal models of alcohol addiction. IC50 value: Target: GABA receptor Acamprosate, or N-acetyl homotaurine, is an N-methyl-D-aspartate approved by the… Purity: 98.0% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 50 mg 100 mg

Allopregnanolone alpha-Asarone (3α,5α-THP; SAGE-547; Brexanolone) Cat. No.: HY-101107 (α-Asarone; trans-Asarone) Cat. No.: HY-N0700

Bioactivity: is a metabolite. Bioactivity: Alpha-Asarone is one of the main psychoactive compounds, and Allopregnanolone is an allosteric modulator of the GABA possesses an antidepressant-like activity in mice. receptor. Used to treat .

Purity: 98.0% Purity: 99.99% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 g, 5 g

Aminooxyacetic acid hemihydrochloride AZD-6280 (Carboxymethoxylamine Hemihydrochloride) Cat. No.: HY-107994 Cat. No.: HY-19872

Bioactivity: hemihydrochloride is a malate-aspartate Bioactivity: AZD-6280 is a selective GABAA(α2/3) receptor modulator, used shuttle ( MAS) inhibitor which also inhibits the GABA for treatment of generalized anxiety disorder. degradating enzyme GABA-T.

Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 1 g

Baclofen Cat. No.: HY-B0007 Cat. No.: HY-100124

Bioactivity: Baclofen is a gamma-amino- (GABA) derivative used Bioactivity: Bamaluzole is a GABA receptor agonist extracted from patent as a skeletal muscle relaxant. Target: GABA Receptor Baclofen, WO 2012064642 A1. a lipophilic analog of gamma-aminobutyric acid, is clinically used to control spasticity. Baclofen pretreatment (3 mg/kg) not only prolonged the time taken for animals to reach a core… Purity: 98.21% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 1 g, 5 g Size: 1 mg, 5 mg

www.MedChemExpress.com 75

Basmisanil (RG1662; RO5186582) Cat. No.: HY-16716 (3-Ethyl-3-methylglutarimide; Bemegrid) Cat. No.: HY-B1326

Bioactivity: is a highly selective GABAAα5 negative allosteric Bioactivity: Bemegride is a central nervous system and antidote modulator. for poisoning.

Purity: 99.49% Purity: 99.91% Clinical Data: Phase 2 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 100 mg, 500 mg

Bifenazate Broflanilide Cat. No.: HY-119687 Cat. No.: HY-108689

Bioactivity: Bifenazate is a carbazate acaricide that control 100% of mites Bioactivity: Broflanilide is a potential insecticide and metabolized to at a concentration of 25 ppm [1]. Bifenazate is a positive desmethyl-broflanilide, which is a potent antagonist at the insect resistant-to- (RDL) GABA receptor, and allosteric modulator of GABA receptor [2]. inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM.

Purity: 99.91% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 100 mg, 500 mg, 1 g

Carburazepam CGP11952 (RGH 3331; Uxepam) Cat. No.: HY-U00241 Cat. No.: HY-U00192

Bioactivity: is a drug which derives from . Bioactivity: CGP11952 is a triazolyl-Benzaphenon resembling the (BZD, BZs) are a class of psychoactive drugs benzodiazepines in its pharmacological action. CGP11952 is an whose core chemical structure is the fusion of a ring experimental benzodiazepine derivative. and a diazepine ring.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

CGP52432 Cat. No.: HY-103531 Cat. No.: HY-B0353

Bioactivity: CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 Bioactivity: Chlormezanone resembles benzodiazepine. The action of nM. Chlormezanone is similar to benzodiazepine-type agents. Chlormezanone is used as an anxiolytic and a muscle relaxant.

Purity: 98.50% Purity: 99.85% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 100 mg

Cholesterol myristate Cirsimaritin (Cholesteryl myristate; Cholesteryl tetradecanoate) Cat. No.: HY-N2338 Cat. No.: HY-N6648

Bioactivity: myristate is a natural steroid present in Bioactivity: Cirsimaritin binds weakly to the benzodiazepine site on

traditional Chinese medicine. Cholesterol myristate binds to GABAA receptors, with antidepressant, anxiolytic and several ion channels such as the nicotinic acetylcholine antinociceptive activities. receptor, GABAA receptor, and the inward-rectifier potassium . Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg Size: 1 mg, 5 mg

76 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

CP-409092 DAA-1106 Cat. No.: HY-101639 Cat. No.: HY-19945

Bioactivity: CP-409092 is a GABA(A) partial agonist, used for the Bioactivity: DAA1106 is a potent and selective ligand for peripheral treatment of anxiety. benzodiazepine receptor (PBR), as a potent and selective agonist at the peripheral benzodiazepine receptor. Target:PBR in vitro: DAA1106 binding to PBR was significantly increased in widespread areas in MCI subjects when compared to healthy… Purity: >98% Purity: 99.96% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 250 mg, 100 mg Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg

Dihydroergotoxine mesylate DL-Borneol ( mesylates) Cat. No.: HY-B0799 ((±)-Borneol) Cat. No.: HY-N1368

Bioactivity: Dihydroergotoxine mesylate is a complex of closely related Bioactivity: DL-Borneol is a racemic mixture of D-Borneol and L-Borneol. alkaloid salts; Binds with high affinity to the GABAA receptor DL-Borneol is widely used for the treatment of cardiovascular Cl- channel, producing an allosteric interaction with the and cerebrovascular diseases in China. benzodiazepine site. IC50 value: Target: Dihydroergotoxine mesylate also interacts with central dopaminergic,… Purity: 98.0% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 1 g, 5 g

DMCM hydrochloride Emamectin Benzoate Cat. No.: HY-100369A (MK-244) Cat. No.: HY-B0837

Bioactivity: DMCM (hydrochloride) is Benzodiazepine inverse agonist that Bioactivity: Emamectin Benzoate (MK-244) works as a displays anxiogenic and potent activity. The activator by binding gamma aminobutyric acid (GABA) receptor reference for administration is ranging 0.4 from 0.8 mg/kg . and glutamate-gated chloride channels disrupting nerve signals DMCM (hydrochloride) was shown to bind to within arthropods. GABAA/benzodiazepine Purity: receptors98.14% in the rat brain with high affinity. DMCM… Purity: 94.77% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 100 mg, 500 mg

Ethyl dirazepate Cat. No.: HY-101596 (HOE 36-801) Cat. No.: HY-16579A

Bioactivity: is a drug which is a benzodiazepine Bioactivity: Etifoxine(HOE 36-801) is potentiator of GABAA receptor derivative. It has anxiolytic and and possibly other function in cultured neurons. Etifoxine preferentially acts on characteristic benzodiazepine properties. β2 or β3 subunit-containing GABAA receptors.

Purity: >98% Purity: 99.94% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Etifoxine hydrochloride (HOE 36-801 (hydrochloride)) Cat. No.: HY-16579 (R 16659) Cat. No.: HY-B0100

Bioactivity: Etifoxine hydrochloride (HOE 36-801 hydrochlorid) is Bioactivity: Etomidate(R-16659) is a GABAA receptors agonist, which is a potentiator of GABAA receptor function in cultured neurons. short acting intravenous anaesthetic agent used for the Etifoxine preferentially acts on β2 or β3 subunit-containing induction of general anaesthesia. GABAA receptors. IC50 value: Target: GABAA receptor Etifoxine exhibits anxiolytic activity in rodents and humans with no… Purity: 99.96% Purity: 99.33% Clinical Data: Phase 3 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

www.MedChemExpress.com 77

Etomidate hydrochloride FG8119 (R16659 hydrochloride) Cat. No.: HY-B0100A (NNC13-8119) Cat. No.: HY-U00233

Bioactivity: Etomidate Hcl(R16659 Hcl) is a GABAA receptors agonist, which Bioactivity: FG8119 is a novel benzodiazepine agonist extracted from patent is a short acting intravenous anaesthetic agent used for the US 4745112 A. induction of general anaesthesia.

Purity: 99.09% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

Flumazenil acid (Ro 15-1788) Cat. No.: HY-B0009 (Ro 15-3890) Cat. No.: HY-118844

Bioactivity: Flumazenil is a competitive GABAA receptor antagonist, used Bioactivity: Flumazenil acid is a metabolite of Flumazenil [1]. Flumazenil in the treatment of benzodiazepine overdoses. is a GABAA receptor antagonist [2].

Purity: 99.98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 50 mg, 100 mg

Fluxametamide Cat. No.: HY-108690 (SR95531) Cat. No.: HY-103533

Bioactivity: Fluxametamide is an insecticide with wide spectrum, acts as an Bioactivity: Gabazine is a selective and competitive antagonist of GABAA antagonist of GABA- and glutamate-gated chloride channels, receptor, with an IC50 of ~0.2 μM for GABA receptor. with IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls.

Purity: 99.74% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

Gidazepam A (Gidasepam; Hidazepam; Hydazepam) Cat. No.: HY-U00315 (BN-52020) Cat. No.: HY-B0355

Bioactivity: is an agonist of GABA receptor channels ( GABA Bioactivity: Ginkgolide A (BN-52020) is an extract from in Ginkgo biloba RCs). and a g-aminobutyric acid (GABA) antagonist.

Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

Ginsenoside Rc hydrochloride (Panaxoside Rc) Cat. No.: HY-N0042 Cat. No.: HY-100809

Bioactivity: Ginsenoside Rc, one of major Ginsenosides from Panax ginseng, Bioactivity: Guvacine hydrochloride is an alkaloid from the nut of Areca

enhances GABA receptor A ( GABAA)-mediated ion channel catechu, acts as an inhibitor of GABA transporter, and currents (I ). Ginsenoside Rc inhibits the expression of dispalys modest selectivity for cloned GABA transporters with GABA IC s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat TNF-α and IL-1β. 50 GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM… Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 5 mg, 10 mg 5 mg, 10 mg

78 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Imepitoin hydrochloride (AWD 131-138) Cat. No.: HY-14953 Cat. No.: HY-100810

Bioactivity: (AWD 131-138) is a new low-affinity partial Bioactivity: Isoguvacine hydrochloride is a GABA receptor agonist. benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.

Purity: 99.52% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 25 mg, 50 mg, 100 mg

Jujuboside A L-655708 Cat. No.: HY-N0659 Cat. No.: HY-14426

Bioactivity: Jujuboside A is a glycoside extracted from Semen Ziziphi Bioactivity: L-655708 is a potent α5 subunit-selective GABAA receptor Spinosae, a Chinese herbal medicine used to treat and inverse agonist (Ki = 0.45 nM). IC50: 0.45 nM (Ki) Target: anxiety. GABA in vitro: L-655708 is a potent, selective inverse agonist for the benzodiazepine site of GABAA receptors containing the α5 subunit (Ki = 0.45 nM). Displays 50-100-fold selectivity… Purity: 98.18% Purity: 99.25% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg 5 mg, 10 mg, 50 mg

L- L-DABA ((S)-4-Amino-3-isoxazolidone; (S)-Cycloserine) Cat. No.: HY-B1122 (L-2,4-Diaminobutyric acid) Cat. No.: HY-101414

Bioactivity: L-cycloserine irreversibly inhibit GABA pyridoxal Bioactivity: L-DABA (L-2,4-Diaminobutyric acid) is a week GABA 5′-phosphate-dependent aminitransferase in E. coli, as well in transaminase inhibitor with an IC50 of larger than 500 μM; the brains of various animals in a time-dependent manner, exhibits antitumor activity in vivo and in vitro. results in increased levels of gamma-aminobutyric acid (GABA), which is an inhibitory neurotransmitter in vivo. Purity: 99.50% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in Water, 10 mg, 50 mg, 100 mg 100 mg

Loreclezole (R 72063) Cat. No.: HY-105272 Cat. No.: HY-19371

Bioactivity: , an antiepileptic compound, is a selective GABAA Bioactivity: Lorediplon is a novel non-benzodiazepine, hypnotic drug acting receptor modulator and acts as a positive allosteric as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep. modulator of β2 or β3-subunit containing receptors [1] [2].

Purity: >98% Purity: 99.78% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Lotilaner Methionine Cat. No.: HY-116564 (MRX-1024; D-Methionine) Cat. No.: HY-13694

Bioactivity: Lotilaner is a parasiticide, acts as a potent non-competitive Bioactivity: Methionine (MRX-1024) is an effective chemoprotective agent

antagonist of insects GABACl receptors, with an IC50 of 23.84 which can also inhibit the neuronal activity through GABAA nM for Drosophila melanogaster GABA receptor. No effect on a receptor activation. dog GABAA receptor [1]. Purity: >98% Purity: 97.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size: 10mM x 1mL in Water, 1 g

www.MedChemExpress.com 79

MRK-016 Cat. No.: HY-100370 (DM9384; DZL-221) Cat. No.: HY-B0340

Bioactivity: MRK-016 is a selective, orally bioavailable inverse agonist of Bioactivity: Nefiracetam is a GABAergic, cholinergic, and

GABAA α5 receptor, with an EC50 of 3 nM for GABA A α5, neuronal systems enhancer for Ro 5-4864-induced convulsions.

and Kis of 0.83, 0.85, 0.77and 1.4nM for humanGABA

Aα1β3γ2, GABA Aα2β3γ2, GABA Aα3β3γ2, and GABA Aα5β3… Purity: 98.29% Purity: 99.96% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 50 mg, 100 mg

NEO 376 NS11394 (SPI-376) Cat. No.: HY-101583 Cat. No.: HY-11048

Bioactivity: NEO 376 is a selective modulator of 5-HT1 receptor, GABA Bioactivity: NS11394 is a potent and subtype-selective GABA(A) receptor and dopamine receptor, with anti-psychotic receptor-positive modulator; possesses a functional efficacy actively. selectivity profile of alpha(5) > alpha(3) > alpha(2) > alpha(1) at GABA(A) alpha subunit-containing receptors.

Purity: >98% Purity: 99.84% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

ONO-8590580 Cat. No.: HY-112788 (ISF2522) Cat. No.: HY-B1715

Bioactivity: ONO-8590580 is a GABAA α5 negative allosteric modulator. Bioactivity: Oxiracetam is a cyclic derivative of γ-aminobutyric acid ( GABA) which has been commonly used as nootropic drug to treat cognitive impairments.

Purity: 99.85% Purity: 99.76% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

p-Hydroxybenzaldehyde Picrotoxin Cat. No.: HY-Y0313 (Cocculin) Cat. No.: HY-101391

Bioactivity: p-Hydroxybenzaldehyde is a one of the major components in Bioactivity: Picrotoxin is a noncompetitive antagonist of GABAA receptor. Dendrocalamus asper bamboo shoots, with antagonistic effect on

GABAA receptor of the α 1β 2γ 2S subtype at high concentrations.

Purity: 98.0% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 g 100 mg

Pipequaline hydrochloride (PK-8165) Cat. No.: HY-100140 (PK-8165 (hydrochloride)) Cat. No.: HY-100140A

Bioactivity: Pipequaline (PK 8165) is a partial benzodiazepine receptor Bioactivity: Pipequaline hydrochloride (PK-8165 hydrochloride) is a partial agonist with anxiolytic activity [1] [2]. benzodiazepine receptor agonist with anxiolytic activity [1] [2].

Purity: 98.61% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg

80 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Primidone Cat. No.: HY-B0339 Cat. No.: HY-B0546

Bioactivity: is an anticonvulsant of the pyrimidinedione class. Bioactivity: Procaine is a drug of the amino ester group, which acts through multiple targets. Target: Others Procaine is a local anesthetic of the ester type that has a slow onset and a short duration of action.Procaine (0.01-100 microM) inhibited the 5-HT3 receptor-mediated inward current in the… Purity: 99.74% Purity: 99.07% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 1 g, 5 g 100 mg

Procaine hydrochloride Cat. No.: HY-B0546A (AC-3933) Cat. No.: HY-106025

Bioactivity: Procaine Hydrochloride is a local anesthetic drug of the amino Bioactivity: Radequinil (AC-3933) is a benzodiazepine receptor (BzR) ester group. Target: Others Procaine is a local anesthetic of partial inverse agonist. AC-3933 binds to GABA(-) and

the ester type that has a slow onset and a short duration of GABA(+) ligand with Kis of 5.15 and 6.11 nM, respectively action.Procaine (0.01-100 microM) inhibited the 5-HT3 [1]. receptor-mediated inward current in the whole-cell patch clamp… Purity: 99.95% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 1 g, 5 g Size: 500 mg, 250 mg

Remimazolam benzenesulfonate (CN-7056 benzenesulfonate) Cat. No.: HY-14867A Cat. No.: HY-106547

Bioactivity: benzenesulfonate is a GABA agonist. Bioactivity: Rilmazafone is a benzodiazepine ω ligand with sedative and hypnotic effects [1].

Purity: 97.78% Purity: >98% Clinical Data: Phase 3 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 500 mg, 100 mg, 250 mg 5 mg, 10 mg, 50 mg, 100 mg

Rilmazafone hydrochloride (450191S) Cat. No.: HY-U00228 (PK 26124) Cat. No.: HY-B0211

Bioactivity: Rilmazafone hydrochloride (450191S) is a benzodiazepine ω Bioactivity: Riluzole is an anticonvulsant drug and belongs to the family ligand with sedative and hypnotic effects [1]. of use-dependent Na+ channel blocker which can also inhibit

GABA uptake with an IC50 of 43 μM.

Purity: >98% Purity: 99.83% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 500 mg, 1 g

Riluzole hydrochloride Ro 41-3290 (PK 26124 hydrochloride) Cat. No.: HY-B0211A Cat. No.: HY-U00215

Bioactivity: Riluzole hydrochloride is an anticonvulsant drug and belongs Bioactivity: Ro 41-3290 is the desethylated derivative of Ro 41-3696, which to the family of use-dependent Na+ channel blocker which can is a partial agonist at the benzodiazepine receptor. Ro 41-3290 is an investigational hypnotic. also inhibit GABA uptake with an IC50 of 43 μM.

Purity: 99.94% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 1 mg, 5 mg, 10 mg, 20 mg 50 mg, 100 mg, 500 mg

www.MedChemExpress.com 81

RO 4938581 Ru-32514 Cat. No.: HY-107489 Cat. No.: HY-19065

Bioactivity: RO 4938581 is a potent and selective GABAA α5 inverse Bioactivity: Ru-32514 is an agonist of benzodiazepine receptor.

agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a

lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a ( Ki, 174, 185, 80 nM, respectively); RO 4938581 is used in the research… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

RWJ-51204 S-8510 phosphate Cat. No.: HY-19308 (SB-737552 phosphate) Cat. No.: HY-103225

Bioactivity: RWJ-51204 is a partial agonist of GABA(A) receptor, with Ki Bioactivity: S-8510 (phosphate) is an inverse Benzodiazepine (BDZ) receptor of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors. agonist, with K is of 34.6 nM, 36.2 nM for –GABA and +GABA respectively.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 250 mg, 500 mg

Sarmazenil SKF89976A hydrochloride (Ro 15-3505) Cat. No.: HY-100248 (d,l-SKF89976A hydrochloride) Cat. No.: HY-100228A

Bioactivity: is a benzodiazepine receptor antagonist. Bioactivity: SKF89976A hydrochloride is a selective GABA transporter (

GAT-1) inhibitor with IC50s of 0.28 μM, 137.34 μM and 202.8 μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively.

Purity: >98% Purity: 98.15% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

SSD114 hydrochloride SX-3228 Cat. No.: HY-103668A Cat. No.: HY-100291

Bioactivity: SSD114 hydrochloride is a novel GABAB receptor positive Bioactivity: SX-3228 is a selective benzodiazepine1 ( BZ1) receptor agonist with an IC of 17 nM. allosteric modulator. 50

Purity: 99.07% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Tiagabine hydrochloride (NO050328 hydrochloride; NO328 (NO050328; NO328; TGB) Cat. No.: HY-B0696 hydrochloride; TGB hydrochloride) Cat. No.: HY-B0696A

Bioactivity: Tiagabine (NO050328) is a potent and selective GABA reuptake Bioactivity: Tiagabine hydrochloride is a potent and selective GABA

inhibitor, used as an anticonvulsant agent, with IC50s of 67, reuptake inhibitor, used as an anticonvulsant agent, with 3 3 IC s of 67, 446 and 182 nM for [ H]GABA uptake in 446 and 182 nM for [ H]GABA uptake in Synaptosomes, Neurons 50 and Glia, respectively [1]. Synaptosomes, Neurons and Glia, respectively [1]. Purity: >98% Purity: 98.20% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg

82 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Tiagabine hydrochloride hydrate (NO050328 hydrochloride TPA 023 hydrate; NO328 hydrochloride hydrate; …) Cat. No.: HY-B0696B Cat. No.: HY-101640

Bioactivity: Tiagabine hydrochloride hydrate is a potent and selective Bioactivity: TPA 023 is a GABAA α2/α3 subtype-selective agonist, with Ki GABA uptake inhibitor, used as an anticonvulsant agent, with of 0.19-0.41 nM. 3 IC50s of 67, 446 and 182 nM for [ H]GABA uptake in Synaptosomes, Neurons and Glia, respectively [1]. Purity: >98% Purity: 99.71% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 20 mg

U-101017 U93631 (PNU 101017) Cat. No.: HY-19250 Cat. No.: HY-100686

Bioactivity: U-101017 is a partial agonist of benzodiazepine receptor and Bioactivity: U93631 is a GABAA receptor ligand of novel chemical structure GABAA receptor, with anxiolytic effects. with IC50 of 100 nM,and has been shown to induce a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAA receptors. target: GABAA receptor IC 50: GABAA receptor[1] In vitro: In the presence of U93631 at 5 UM,… Purity: >98% Purity: 99.92% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Uldazepam (U31920) Cat. No.: HY-100264 (γ-Vinyl-GABA) Cat. No.: HY-15399

Bioactivity: is a benzodiazepine derivative and can be used to Bioactivity: Vigabatrin(γ-Vinyl-GABA; Sabril) is a structural analog of the treat patients with anxiety syndromes as tranquilizer. inhibitory neurotransmitter γ-aminobutyric acid (GABA) that irreversibly inhibits the catabolism of GABA by GABA transaminase. IC50 value: Target: GABA transaminase Clinical studies have shown that vigabatrin is superior to in… Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in Water, 5 mg, 10 mg, 50 mg, 100 mg

Vigabatrin Hydrochloride (γ-Vinyl-GABA hydrochloride) Cat. No.: HY-B0033 (SAGE-217) Cat. No.: HY-103040

Bioactivity: Vigabatrin Hcl(γ-Vinyl-GABA; Sabril) is a structural analog of Bioactivity: Zuranolone (SAGE-217) is a potent GABAA receptor agonist the inhibitory neurotransmitter γ-aminobutyric acid (GABA) with EC s of 296 and 163 nM for α β γ and α β δ that irreversibly inhibits the catabolism of GABA by GABA 50 1 2 2 4 3 GABA receptors, respectively. transaminase. IC50 value: Target: GABA transaminase Clinical A studies have shown that vigabatrin is superior to placebo in… Purity: 98.0% Purity: 99.93% Clinical Data: Launched Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

γ-Aminobutyric acid (4-Aminobutyric acid) Cat. No.: HY-N0067

Bioactivity: γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain [1] [2] , binding to the ionotropic GABA receptors ( GABAA

receptors) and metabotropic receptors ( GABAB receptors Purity: 97.0% Clinical Data: No Development Reported Size: 10mM x 1mL in Water, 100 mg

www.MedChemExpress.com 83 GlyT transporters

Glycine transporters (GlyTs) belong to a large family of Na+/Cl- -dependent transporter proteins that includes transporters for monoamines [5-hydroxytryptamine (serotonin), noradrenaline and dopamine] and γ-aminobutyric acid. GlyT-mediated glycine uptake is energetically coupled with the transmembrane sodium gradient maintained by the Na+/K+-ATPase. GlyT1 is essential for regulating glycine concentrations at synaptic receptors. GlyT2 is uniquely designed for neurotransmitter recycling at inhibitory synapses, and loss of GlyT2 function generates a severely hyperexcited state.

84 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] GlyT Inhibitors & Modulators

Bitopertin R enantiomer (RG1678; RO4917838) Cat. No.: HY-10809 (RG1678 (R enantiomer); RO4917838 (R enantiomer)) Cat. No.: HY-10809A

Bioactivity: Bitopertin is a potent, noncompetitive glycine reuptake Bioactivity: Bitopertin R enantiomer (RG1678 R enantiomer; RO4917838 R inhibitor, inhibits glycine uptake at human GlyT1 with a enantiomer) is the R-enantiomer of Bitopertin. Bitopertin is a concentration exhibiting IC50 of 25 nM. potent, noncompetitive glycine reuptake inhibitor, inhibits glycine uptake at human GlyT1 with a concentration exhibiting IC50 of 25 nM. Purity: 99.75% Purity: 95.00% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 1 mg

GlyT1 Inhibitor 1 LY2365109 hydrochloride Cat. No.: HY-112432 Cat. No.: HY-100416A

Bioactivity: GlyT1 Inhibitor 1 is a potent and selective GlyT1 inhibitor Bioactivity: LY2365109 is a potent and selective GlyT1 inhibitors with IC50 [1] value of 15.8 nM. target: GlyT1[1] IC 50: 15.8 nM [1] In vivo: with an IC50 of 38 nM for rGlyT1 . Antipsychotic activity The reference for LY2365109 is 0.3 or 30 mg/kg by PO. [1] . LY2365109 appeared slightly more potent than ALX5407 over the dose-range tested on CSF levels of glycine in the rat… Purity: >98% Purity: 98.83% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

MPDC (Methylglycine; N-Methylaminoacetic acid; Sarcosin; Cat. No.: HY-101334 Sarcosinic acid) Cat. No.: HY-101037

Bioactivity: MPDC is a potent and competitive inhibitor of the Bioactivity: Sarcosine is a type 1 ( GlyT) inhibitor and Na+-dependent high-affinity glutamate transporter in an N-methyl-D-aspartate ( NMDA) receptor co-agonist at the forebrain synaptosomes [1]. glycine binding site.

Purity: Purity: 97.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg 100 mg

Tilapertin Yoda 1 (AMG747) Cat. No.: HY-19887 (GlyT2-IN-1) Cat. No.: HY-18723

Bioactivity: Tilapertin is an oral inhibitor of glycine transporter type-1 Bioactivity: Yoda 1 is a glycine transporters GLYT2 inhibitor. ( GlyT1).

Purity: >98% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 85 iGluR Ionotropic glutamate receptors

iGluR (ionotropic ) is a ligand-gated ion channel that is activated by the neurotransmitter glutamate. iGluR are integral membrane proteins compose of four large subunits that form a central ion channel pore. Sequence similarity among all known glutamate receptor subunits, including the AMPA, kainate, NMDA, and δ receptors. AMPA receptors are the main charge carriers during basal transmission, permitting influx of sodium to depolarise the postsynaptic membrane. NMDA receptors are blocked by magnesium ions and therefore only permit ion flux following prior depolarisation. This enables them to act as coincidence detectors for synaptic plasticity. Calcium influx through NMDA receptors leads to persistent modifications in the strength of synaptic transmission.

86 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] iGluR Inhibitors & Modulators

(-)- (-)- Maleate ((R)-Aspartic acid; D-(-)-Aspartic acid) Cat. No.: HY-42068 ((-)-MK 801 (Maleate)) Cat. No.: HY-15084A

Bioactivity: (-)-Aspartic acid is an endogenous NMDA receptor agonist. Bioactivity: (-)-Dizocilpine ((-)-MK 801) Maleate is the enantiomer of (+)-MK-801. (+)-MK 801 Maleate is a potent, selective and non-competitive NMDA receptor antagonist.

Purity: 97.0% Purity: 99.70% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 5 g 10 mg, 50 mg

(S)-(-)-5-Fluorowillardiine (S)-(-)-5-Fluorowillardiine hydrochloride ((5S)-Fluorowillardiine; (S)-5-Fluorowillardiine) Cat. No.: HY-16713 ((5S)-Fluorowillardiine hydrochloride; …) Cat. No.: HY-16713A

Bioactivity: (S)-(-)-5-Fluorowillardiine is a potent and specific AMPAR Bioactivity: (S)-(-)-5-Fluorowillardiine Hcl is a potent and specific AMPAR agonist. agonist.

Purity: >98% Purity: 99.82% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mg, 50 mg Size: 10mM x 1mL in Water, 10 mg, 50 mg

(S)- 1-BCP ((-)-Willardiine) Cat. No.: HY-12499 (Piperonylic acid piperidide) Cat. No.: HY-101363

Bioactivity: (S)-Willardiine is a potent agonist of AMPA/kainate receptors Bioactivity: 1-BCP is a centrally active drug that modulates AMPA with EC50 of 44.8 uM. IC50 value: 44.8 uM(EC50) [1] Target: receptor gated currents. 1-BCP is a memory-enhancing agent AMPA/ agonist in vitro: The (S)- but not [1] [2]. (R)-isomers of willardiine and 5-bromowillardiine were potent agonists, producing rapidly but incompletely desensitizing… Purity: 98.70% Purity: 99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 5 mg

24-Hydroxycholesterol 6-Methoxy-2-naphthoic acid Cat. No.: HY-N2370 ( impurity O) Cat. No.: HY-B2121

Bioactivity: 24-Hydroxycholesterol is a natural sterol, which serves as a Bioactivity: 6-Methoxy-2-naphthoic acid is an NMDA receptor modulator positive allosteric modulator of N-Methyl-d-Aspartate extracted from patent WO 2012019106 A2. (NMDA) receptorsR, and a potent activator of the transcription factors LXR.

Purity: 98.0% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 2 mg, 5 mg Size: 10mM x 1mL in DMSO, 100 mg

7-Chloro-4-hydroxyquinoline-2-carboxylic acid 7-Chlorokynurenic acid sodium salt (7-Chlorokynurenic acid) Cat. No.: HY-100811 Cat. No.: HY-100811A

Bioactivity: 7-Chloro-4-hydroxyquinoline-2-carboxylic acid Bioactivity: 7-Chlorokynurenic acid sodium salt is a selective antagonist (7-Chlorokynurenic acid) is a selective antagonist at the at the glycine modulatory site of the N-methyl-D-aspartate glycine modulatory site of the N-methyl-D-aspartate receptor complex and also a potent inhibitor of the reuptake

receptor complex and also a potent inhibitor of the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM. of glutamate into synaptic vesicles with a Ki of 0.59 μM. Purity: 99.62% Purity: 99.79% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 87

AMPA Receptor Modulator-1 Ampalex Cat. No.: HY-112699 (CX516; BDP 12; CX516) Cat. No.: HY-10933

Bioactivity: AMPA Receptor Modulator-1 is a potent, oral active and Bioactivity: Ampalex (Ampakine CX516; CX516; BDP 12) is an ampakine and selective AMPAR regulatory protein TARP γ-8 negative nootropic that acts as an AMPA receptor positive allosteric

modulator with a p IC50 of 9.7, more selective over GluA1/γ-2 modulator as a treatment for Alzheimer's disease, [1] schizophrenia and mild cognitive impairment (MCI). (pIC 50=5) . Purity: >98% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 100 mg, 500 mg, 250 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg, 200 mg

Aniracetam (Ro 13-5057) Cat. No.: HY-10932 (NRX-1074; AGN-241660) Cat. No.: HY-102053

Bioactivity: (Ro 13-5057) is a and neuroprotective Bioactivity: Apimostinel is an oral NMDA receptor partial agonist. drug, which is selectively modulates the AMPA receptor and nAChR.

Purity: 99.43% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 5 mg, 10 mg, 25 mg

Becampanel BMS-986163 (AMP 397) Cat. No.: HY-15073 Cat. No.: HY-107774

Bioactivity: (AMP397) is the first competitive AMPA Bioactivity: BMS-986163 is a negative allosteric modulator of GluN2B. The antagonist and an antiepileptic agent. prodrug BMS-986163 rapidly converts to its active parent

molecule BMS-986169 ( Ki=4 nM, IC50=24 nM).

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 500 mg, 250 mg

CFM-2 CIQ Cat. No.: HY-12503 Cat. No.: HY-18699

Bioactivity: CFM-2 is a selective non-competitive AMPAR antagonist. Bioactivity: CIQ is a subunit-selective potentiator of NMDA receptors containing the NR2C or NR2D subunit.

Purity: 98.32% Purity: 99.48% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 25 mg

CMPDA CNQX Cat. No.: HY-12508 (FG9065) Cat. No.: HY-15066

Bioactivity: CMPDA is a positive allosteric modulator of AMPA receptors Bioactivity: CNQX (FG9065) is a potent AMPA/kainate receptor antagonist. with EC50s of 45.4 ± 4.2 nM/63.4 ± 5.6 nM for GluA2i/GluA2o receptor.

Purity: 98.0% Purity: 98.05% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

88 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

CNS-5161 hydrochloride (CNS 5161A) Cat. No.: HY-101809 (MKC-231) Cat. No.: HY-17553

Bioactivity: CNS-5161 hydrochloride is a novel NMDA ion-channel Bioactivity: Coluracetam(MKC-231) is a new choline uptake enhancer. IC50 antagonist that interacts with the NMDA receptor/ion value: Target: in vitro: MKC-231 (10(-10)-10(-6) moll) channel site to produce a noncompetitive blockade of the significantly increased high affinity choline uptake (HACU) actions of glutamate. when it was incubated with the hippocampal synaptosomes of ethylcholine mustard aziridinium ion (AF64A) treated rats, but… Purity: >98% Purity: 99.77% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

CX546 D-AP5 Cat. No.: HY-12505 (D-APV; D-2-Amino-5-phosphonovaleric acid) Cat. No.: HY-100714A

Bioactivity: CX546 is a selective positive AMPAR modulator; the Bioactivity: D-AP5 is a NMDA receptor antagonist. prototypical ampakine agent. IC50 value: Target: AMPAR agonist in vitro: Treatments with the ampakine CX614 markedly and reversibly increased brain-derived neurotrophic factor (BDNF) mRNA and protein levels in cultured rat entorhinal/hippocampal… Purity: 99.50% Purity: 95.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mg, 50 mg Size: 10mM x 1mL in Water, 5 mg, 10 mg

Dizocilpine Maleate DNQX ((+)-MK 801 (Maleate)) Cat. No.: HY-15084 (FG 9041) Cat. No.: HY-15067

Bioactivity: Dizocilpine ((+)-MK 801) Maleate is a potent, selective and Bioactivity: DNQX (FG 9041) is a AMPA receptor antagonists.

non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.

Purity: 99.98% Purity: 98.45% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 25 mg, 50 mg, 100 mg, 200 mg

Dynorphin A (1-10) TFA A 1-10 Cat. No.: HY-P1594A Cat. No.: HY-P1594

Bioactivity: (1-10) (TFA), an endogenous opioid neuropeptide, Bioactivity: Dynorphin A (1-10) an endogenous opioid neuropeptide, binds to binds to extracellular loop 2 of the κ-opioid receptor. extracellular loop 2 of the κ-opioid receptor. Dynorphin A

Dynorphin A (1-10) (TFA) also blocks NMDA-activated current (1-10) also blocks NMDA-activated current with an IC50 of with an IC of 42.0 μM. 50 42.0 μM.

Purity: 95.04% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg

Eliprodil (SL-820715) Cat. No.: HY-12881 (ZK200775; MPQX) Cat. No.: HY-15069

Bioactivity: (SL-820715) is a non-competitive NR2B-NMDA receptor Bioactivity: Fanapanel (ZK200775) is a highly selective AMPA/kainate antagonist(IC50=1 uM), less potent for NR2A- and antagonist with little activity against NMDA; have Ki values NR2C-containing receptors(IC50> 100 uM). of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.

Purity: 99.67% Purity: 99.93% Clinical Data: Phase 2 Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 10 mg, 50 mg

www.MedChemExpress.com 89

Fanapanel hydrate (ZK200775 (hydrate); MPQX hydrate) Cat. No.: HY-15069A (CX-691; Org24448) Cat. No.: HY-10937

Bioactivity: Fanapanel hydrate (ZK200775 hydrate) is a highly selective Bioactivity: Farampator (CX-691;Org24448) is an AMPA receptor positive AMPA/kainate antagonist with little activity against NMDA; modulator. have Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.

Purity: 98.98% Purity: 98.90% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Felbamate hydrate (W-554; ADD-03055) Cat. No.: HY-B0184 (W-554 (hydrate); ADD-03055 (hydrate)) Cat. No.: HY-B0184A

Bioactivity: Felbamate (W-554) is a potent nonsedative anticonvulsant whose Bioactivity: Felbamate (hydrate) (W-554 (hydrate)) is a potent nonsedative clinical effect may be related to the inhibition of anticonvulsant whose clinical effect may be related to the N-methyl-D-aspartate (NMDA). inhibition of N-methyl-D-aspartate (NMDA) .

Purity: 98.30% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 10 mg, 50 mg, 100 mg, 200 mg

Flupirtine Maleate (D 9998) Cat. No.: HY-17001A Cat. No.: HY-17001

Bioactivity: Flupirtine(D 9998) is a selective neuronal potassium channel Bioactivity: Flupirtine Maleate(D 9998) is a selective neuronal potassium opener that also has NMDA receptor antagonist properties. that also has NMDA receptor antagonist properties. IC50 Value: Target: Potassium channel; NMDA receptor in vitro: High concentrations of flupirtine antagonized inward currents to NMDA(200 microM) at -70 mV with… Purity: >98% Purity: 99.97% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg, 100 mg, 500 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg, 500 mg

gamma-DGG Glycine (γDGG; γ-D-Glutamylglycine) Cat. No.: HY-100785 Cat. No.: HY-Y0966

Bioactivity: gamma-DGG is a competitive AMPA receptor blocker. Bioactivity: Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.

Purity: 98.08% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 g

GNE 0723 GNE 5729 Cat. No.: HY-108337 Cat. No.: HY-107409

Bioactivity: GNE 0723 is a brain permeable positive allosteric modulator of Bioactivity: GNE 5729 is a brain permeable positive allosteric modulator of

NMDAR, with an EC50 of 21 nM for GluN2A, 7.4 and 6.2 μM NMDAR, with an EC50 of 37 nM for GluN2A, 4.7 and 9.5 μM for GluN2C and GluN2D, respectively. for GluN2C and GluN2D, respectively.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 250 mg, 500 mg

90 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

GV-196771A GYKI53655 hydrochloride Cat. No.: HY-19243 Cat. No.: HY-103228

Bioactivity: GV-196771A is the sodium salt form of GV196771, is an NMDA Bioactivity: GYKI53655 hydrochloride is an receptor antagonist. α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid ( AMPA) antagonist.

Purity: >98% Purity: 99.01% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Ibotenic acid IC87201 ((RS)-; DL-Ibotenic acid) Cat. No.: HY-N2311 Cat. No.: HY-100457

Bioactivity: Ibotenic acid has agonist activity at both the Bioactivity: IC87201, an inhibitor of PSD95-nNOS protein-protein N-methyl-D-aspartate ( NMDA) and trans-ACPD or interactions, suppresses NMDAR-dependent NO and cGMP

metabolotropic quisqualate (Q m) receptor sites. formation.

Purity: 98.27% Purity: 95.53% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Ifenprodil tartrate JNJ-61432059 Cat. No.: HY-12882A Cat. No.: HY-111751

Bioactivity: tartrate is a NR2B subunit selective NMDA Bioactivity: JNJ-61432059 is an oral active and selective negative modulator of AMPAR associated with trans-membrane AMPAR receptor antagonist with an IC50 of 0.3 μM. regulatory protein (TARP) γ-8, with a pIC50 of 9.7 for GluA1/γ-8. Exhibits time- and dose-dependent AMPAR/γ-8 receptor occupancy in mouse hippocampus, resulting in robust… Purity: 97.61% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 50 mg, 100 mg

Kynurenic acid sodium (Quinurenic acid) Cat. No.: HY-100806 Cat. No.: HY-107512

Bioactivity: Kynurenic acid, an endogenous metabolite, is a Bioactivity: Kynurenic acid sodium, an endogenous tryptophan metabolite, is broad-spectrum antagonist targeting NMDA, glutamate, a broad-spectrum antagonist targeting NMDA, α7 nicotinic . Kynurenic acid is also a glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid selective ligand of the GPR35 receptor. sodium is also a selective ligand of the GPR35 receptor.

Purity: 98.75% Purity: 98.60% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 100 mg 100 mg, 500 mg

L-701324 L- monosodium salt Cat. No.: HY-18698 (Monosodium glutamate) Cat. No.: HY-14608A

Bioactivity: L-701324 is an orally active and long acting anticonvulsant Bioactivity: L-Glutamic acid monosodium salt acts as an excitatory with high affinity and selectivity for the glycine site on the transmitter and an agonist at all subtypes of glutamate NMDA receptor. Target: NMDA Receptor L-701324 is a potent, receptors (metabotropic, kainate, NMDA, and AMPA). active anticonvulsant with a reduced propensity to activate (S)-Glutamic acid shows a direct activating effect on the mesolimbic dopaminergic systems in rodents. L-701324 exhibits… release of DA from dopaminergic terminals. Purity: 99.99% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 10 mg, 50 mg 100 mg, 500 mg

www.MedChemExpress.com 91

Linalool LY450108 Cat. No.: HY-N0368 Cat. No.: HY-10935

Bioactivity: Linalool is natural monoterpene in essential olis of Bioactivity: LY450108 is an coriander, acts as a competitive antagonist of Nmethyl alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid d-aspartate (NMDA) receptor, with anti-tumor, (AMPA) receptor potentiator. IC50 value: Target: AMPA anti-cardiotoxicity activity [1]. receptors mediate most of the excitatory neurotransmission and play a key role in synaptic plasticity in the mammalian… Purity: >98% Purity: 99.51% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

MDL 105519 MDL-29951 Cat. No.: HY-15085 Cat. No.: HY-16312

Bioactivity: MDL 105519 is a potent and selective antagonist of glycine Bioactivity: MDL-29951 is a novel glycine antagonist of NMDA receptor binding to the NMDA receptor. 3 activation, with Ki of 0.14 μM for [ H]glycine binding in vitro and in vivo.

Purity: 98.60% Purity: 98.50% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

Meclofenoxate hydrochloride hydrochloride Cat. No.: HY-17555 (D-145 (hydrochloride)) Cat. No.: HY-B0365A

Bioactivity: hydrochloride, an ester of Bioactivity: Memantine (hydrochloride) (D-145 (hydrochloride)), an (DMAE) and 4-chlorophenoxyacetic acid (pCPA), has been shown derivative with low to moderate-affinity for NMDA

to improve memory, have a mentally stimulating effect, and receptors, inhibit CYP2B6 and CYP2D6 with K i of 0.51 nM and improve general cognition. 94.9 μM, respectively.

Purity: 98.32% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 100 mg 1 g, 5 g

Mephenesin Cat. No.: HY-B1283 (LY451395) Cat. No.: HY-10934

Bioactivity: is an NMDA receptor antagonist, is a centrally Bioactivity: Mibampator (LY451395) is a potent and highly selective acting muscle relaxant. potentiator of the AMPA receptors.

Purity: 99.20% Purity: 99.47% Clinical Data: Launched Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g 5 mg, 10 mg, 50 mg, 100 mg

MRZ 2-514 Naspm Cat. No.: HY-101620 (1-Naphthylacetyl ) Cat. No.: HY-12506

Bioactivity: MRZ 2-514 is an antagonist of the -insensitive Bioactivity: Naspm (1-Naphthyl acetyl spermine), a synthetic analogue of

modulatory site of the NMDA receptor (glycineB), with Ki Joro spider , is a calcium permeable AMPA ( CP-AMPA) of 33 μM. receptors antagonist.

Purity: >98% Purity: 96.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

92 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Naspm trihydrochloride NBQX (1-Naphthylacetyl spermine trihydrochloride) Cat. No.: HY-12506A (FG9202) Cat. No.: HY-15068

Bioactivity: Naspm trihydrochloride (1-Naphthylacetyl spermine Bioactivity: NBQX is a highly selective and competitive AMPA receptor trihydrochloride), a synthetic analogue of Joro spider toxin, antagonist. is a calcium permeable AMPA ( CP-AMPA) receptors antagonist.

Purity: 98.0% Purity: 99.99% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Neu2000 NMDA Cat. No.: HY-106408 (N-Methyl-D-aspartic acid) Cat. No.: HY-17551

Bioactivity: Neu2000 is an uncompetitive N-methyl-D-aspartate ( NMDA) Bioactivity: NMDA is a specific agonist for NMDA receptor receptor antagonist. mimicking the action of glutamate, the neurotransmitter which normally acts at that receptor.

Purity: 99.09% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg 50 mg, 100 mg

NMDA-IN-1 NMDAR antagonist 1 Cat. No.: HY-12962 Cat. No.: HY-111500

Bioactivity: NMDA-IN-1 is a potent and NR2B-selective NMDA antagonist with Bioactivity: NMDAR antagonist 1 is a potent and orally bioavailable Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM; no activities NR2B-selective NMDAR antagonist [1]. on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

NT 13 Omberacetam (TPPT) Cat. No.: HY-P7060 (GVS-111; SGS-111) Cat. No.: HY-17456

Bioactivity: NT 13 (TPPT) is a having the amino acid sequence Bioactivity: Omberacetam (GVS-111) is a medication promoted and prescribed L-threonyl-L-prolyl-L-prolyl-L-threonine amide. NT 13 is a in Russia and neighbouring countries as a nootropic. partial N-methyl-D-aspartate receptor ( NMDAR) agonist used in the study of depression, anxiety, and other related diseases. Purity: >98% Purity: 99.85% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Org-26576 citrate Cat. No.: HY-101216 Cat. No.: HY-B0369A

Bioactivity: Org-26576 is a AMPA receptor positive allosteric modulator. Bioactivity: Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker.

Purity: 99.81% Purity: 99.73% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 100 mg

www.MedChemExpress.com 93

Orphenadrine hydrochloride PEAQX Cat. No.: HY-B1126 (NVP-AAM077) Cat. No.: HY-12294

Bioactivity: Orphenadrine hydrochloride is an uncompetitive Bioactivity: PEAQX(NVP-AAM 077) is a potent and orally active NMDA N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 6.0 antagonist with a 15-fold preference for human NMDA receptors ±0.7 μM. with the 1A/2A(IC50=270 nM), rather than 1A/2B(29,600 nM). IC50 value: 270 nM(hNMDA A1/A2) [1] Target: NR2A antagonist in vitro: PEAQX has a high binding affinity for NMDA receptors… Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 100 mg Size: 5 mg, 10 mg, 50 mg

PEAQX tetrasodium hydrate PEPA (NVP-AAM077 tetrasodium hydrate) Cat. No.: HY-12294A Cat. No.: HY-12509

Bioactivity: PEAQX tetrasodium hydrate (NVP-AAM077 tetrasodium hydrate) is Bioactivity: PEPA is an allosteric modulator of AMPA receptors; binds to a potent and orally active NMDA antagonist with a 15-fold the GluA2o and GluA3o LBDs and can be utilized as an indicator preference for human NMDA receptors with the 1A/2A(IC50=270 of AMPA receptor heterogeneity. nM), rather than 1A/2B(29,600 nM). IC50 value: 270 nM(hNMDA A1/A2) [1] Target: NR2A antagonist in vitro: PEAQX has a high… Purity: 98.22% Purity: 98.81% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg

PF-4778574 74 dihydrochloride Cat. No.: HY-14451 (PhTx 74 dihydrochloride) Cat. No.: HY-104020A

Bioactivity: PF-4778574 is a positive allosteric modulation of AMPA Bioactivity: Philanthotoxin 74 dihydrochloride (PhTx 74) is an AMPAR

receptor with EC50 of 45 to 919 nM in differenct cells. antagonist; inhibits GluR3 and GluR1 with IC50s of 263 and 296 nM, respectively.

Purity: >98% Purity: 98.89% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg

Piracetam hydrochloride (UCB-6215) Cat. No.: HY-B0585 ((±)-Procyclidine hydrochlorid) Cat. No.: HY-B1487

Bioactivity: (UCB-6215) is a cyclic derivative of the Bioactivity: Procyclidine hydrochloride is a potent anti-cholinergic agent, neurotransmitter gamma-aminobutyric acid (GABA), used in and is also known to have NMDA antagonist properties. treatment of a wide range of cognitive disorders.

Purity: 99.0% Purity: 99.55% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 100 mg

QNZ46 Radiprodil Cat. No.: HY-15703 (RGH-896) Cat. No.: HY-14777

Bioactivity: QNZ46 is a NR2C/NR2D-selective NMDA receptor non-competitive Bioactivity: Radiprodil (RGH-896) is an orally active and selective NMDA antagonist (IC50 values are 3, 6, 229, and >300, >300 μM NR2B antagonist. A potential therapeutic agent in treatment for NR2D, NR2C, NR2A, NR2B, and GluR1, respectively). IC50 of and possibly other chronic pain conditions value: 3 μM (for NR2D), 6 μM (for NR2C), 229 μM (for NR2D [1]. NR2A) Target: NR2D, NR2C, NR2A in vitro: QNZ46 is a… Purity: 98.89% Purity: 99.26% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

94 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate; (GLYX-13; Thr-Pro-Pro-Thr-NH2) Cat. No.: HY-16728 Thr-Pro-Pro-Thr-NH2 Trifluoroacetate) Cat. No.: HY-16728B

Bioactivity: Rapastinel (GLYX-13) is an N-methyl-D-aspartate receptor Bioactivity: Rapastinel Trifluoroacetate is an NMDA receptor modulator (NMDAR) modulator that has characteristics of a glycine site with glycine-site partial agonist properties and currently in partial agonist. Target: NMDA Rapastinel is a robust cognitive a phase II clinical development program as an adjunctive enhancer and facilitates hippocampal long-term potentiation therapy for major depressive disorder. (LTP) of synaptic transmission in slices. Purity: 99.49% Purity: 98.0% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 25 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg

Rislenemdaz Ro 25-6981 (MK-0657; CERC-301) Cat. No.: HY-106441A Cat. No.: HY-13993

Bioactivity: Rislenemdaz (CERC-301) is an orally bioavailable and selective Bioactivity: Ro 25-6981 is a potent and selective activity-dependent N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B) blocker of NMDA receptors containing the NR2B subunit. IC50

antagonist with Ki and IC 50 of 8.1 nM and 3.6 nM, values are 0.009 and 52 μM for cloned receptor subunit respectively. combinations NR1C/NR2B and NR1C/NR2A respectively.

Purity: 98.01% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Ro 25-6981 Maleate RPR104632 Cat. No.: HY-13993A Cat. No.: HY-101600

Bioactivity: Ro 25-6981 Maleate is a potent and selective Bioactivity: RPR104632 is a specific antagonist of NMDA receptor, with activity-dependent blocker of NMDA receptors containing the potent neuroprotective properties. NR2B subunit. IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively. IC50 value: 9 nM [1] Target: NMDA receptor… Purity: 97.96% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 50 mg, 100 mg

SDZ 220-581 SDZ 220-581 Ammonium salt Cat. No.: HY-13059 Cat. No.: HY-13059A

Bioactivity: SDZ 220-581 is a potent, competitive antagonist at the NMDA Bioactivity: SDZ 220-581 ammonium salt is a potent, competitive antagonist glutamate receptor subtype(pKi= 7.7). at the NMDA glutamate receptor subtype(pKi= 7.7). IC50 Value: Target: NMDA receptor in vitro: Wake-promoting doses of LSN2463359 and LSN2814617 attenuated deficits in performance induced by the competitiveNMDA receptor antagonist SDZ 220,581… Purity: 98.15% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 10 mg, 50 mg

SDZ 220-581 hydrochloride Cat. No.: HY-13059B (DM-235) Cat. No.: HY-17550

Bioactivity: SDZ 220-581 hydrochloride is a potent, competitive antagonist Bioactivity: Sunifiram (DM-235) is a piperazine derived ampakine-like drug at the NMDA glutamate receptor subtype(pKi= 7.7). IC50 Value: which has nootropic effects in animal studies with Target: NMDA receptor in vitro: Wake-promoting doses of significantly higher potency than piracetam. LSN2463359 and LSN2814617 attenuated deficits in performance induced by the competitiveNMDA receptor antagonist SDZ 220,581… Purity: 99.69% Purity: 99.82% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg

www.MedChemExpress.com 95

SYM 2081 SYM2206 Cat. No.: HY-101310 Cat. No.: HY-18689

Bioactivity: SYM 2081 is a high-affinity ligand and potent, selective Bioactivity: SYM 2206 is a novel, potent, non-competitive AMPA receptor agonist of kainate receptors, inhibits [ 3H]-kainate binding antagonist.

with an IC50 of 35 nM, almost 3000- and 200-fold selectivity for kainate receptors over AMPA and NMDA recept… Purity: 97.0% Purity: 99.72% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg 5 mg, 10 mg, 50 mg

Talampanel Transcrocetin (GYKI-53773; LY-300164) Cat. No.: HY-15079 (trans-) Cat. No.: HY-N2072

Bioactivity: is a potent and selective AMPA-receptor antagonist, Bioactivity: Transcrocetin (trans-Crocetin), extracted from ( Crocus is a potential new antiepileptic drug (AED). sativus L.), acts as an NMDA receptor antagonist with high affinity.

Purity: 98.59% Purity: 98.60% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg 5 mg, 10 mg, 50 mg, 100 mg

Transcrocetin meglumine salt Transcrocetinate disodium (trans-Crocetin meglumine salt) Cat. No.: HY-42937 (Disodium trans-crocetinate) Cat. No.: HY-16502

Bioactivity: Transcrocetin meglumine salt, extracted from saffron ( Crocus Bioactivity: Transcrocetinate disodium, extracted from saffron ( Crocus sativus L.), acts as an NMDA receptor antagonist with high sativus L.), acts as an NMDA receptor antagonist with high affinity. affinity.

Purity: 95.13% Purity: 95.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg

Traxoprodil Tulrampator Cat. No.: HY-W018061 (CX-1632) Cat. No.: HY-109046

Bioactivity: (CP101,606) is a potent and selective NMDA Bioactivity: Tulrampator (CX-1632) is an orally bioavailable positive AMPAR (allosteric modulator of AMPA receptor). antagonist and protect hippocampal neurons with an IC50 of 10 [1] nM. Antidepressant .

Purity: 99.43% Purity: 99.40% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

UK-240455 ZL006 Cat. No.: HY-19391 Cat. No.: HY-100456

Bioactivity: UK-240455 is a potent and selective N-methyl D-aspartate ( Bioactivity: ZL006 is a potent inhibitor of nNOS/PSD-95 interaction, and NMDA) glycine site antagonist. inhibits NMDA receptor-mediated NO synthesis.

Purity: >98% Purity: 99.81% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

96 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Zonampanel (YM 872) Cat. No.: HY-15072

Bioactivity: (YM 872) is a selective antagonist of the glutamate receptor subtype, α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor.

Purity: >98% Clinical Data: Phase 2 Size: 1 mg, 5 mg, 10 mg, 20 mg

www.MedChemExpress.com 97 Imidazoline Receptor

Imidazoline receptors are the primary receptors on which and other imidazolines act. There are three classes of imidazoline receptors: I1 receptor – mediates the sympatho-inhibitory actions of imidazolines to lower , (NISCH or IRAS, imidazoline receptor antisera selected), I2 receptor - an allosteric binding site of monoamine oxidase and is involved in pain modulation and neuroprotection, I3 receptor - regulates insulin secretion from pancreatic beta cells. Activated I1-imidazoline receptors trigger the hydrolysis of into DAG. Elevated DAG levels in turn trigger the synthesis of second messengers and downstreameicosanoids. In addition, the sodium- antiporter is inhibited, and enzymes of catecholamine synthesis are induced. The I1-imidazoline receptor may belong to the neurocytokine receptorfamily, since its signaling pathways are similar to those of interleukins.

98 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Imidazoline Receptor Inhibitors & Modulators

Agmatine sulfate Allantoin Cat. No.: HY-101238 (5-Ureidohydantoin) Cat. No.: HY-N0543

Bioactivity: sulfate exerts modulatory action at multiple Bioactivity: Allantoin is a skin conditioning agent that promotes healthy molecular targets, such as neurotransmitter systems, ion skin, stimulates new and healthy tissue growth. channels and synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor. Purity: 98.0% Purity: 98.36% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg, 1 g 100 mg

Moxonidine Moxonidine hydrochloride (BDF5895) Cat. No.: HY-B0374 (BDF5895 hydrochloride) Cat. No.: HY-B0374A

Bioactivity: Moxonidine is a selective agonist at the imidazoline receptor Bioactivity: Moxonidine Hydrochloride is a selective agonist at the subtype 1, used as antihypertensive agent. imidazoline receptor subtype 1, used as antihypertensive agent.

Purity: 99.91% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 99 mAChR Muscarinic acetylcholine receptor

mAChRs (muscarinic acetylcholine receptors) are acetylcholine receptors that form G protein-receptor complexes in the cell membranes of certainneurons and other cells. They play several roles, including acting as the main end-receptor stimulated by acetylcholine released from postganglionic fibersin the parasympathetic nervous system. mAChRs are named as such because they are more sensitive to than to . Their counterparts are nicotinic acetylcholine receptors (nAChRs), receptor ion channels that are also important in the autonomic nervous system. Many drugs and other substances (for example pilocarpineand scopolamine) manipulate these two distinct receptors by acting as selective agonists or antagonists. Acetylcholine (ACh) is a neurotransmitter found extensively in the brain and the autonomic ganglia.

100 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] mAChR Inhibitors & Modulators

(+)- hydrochloride hemihydrate (-)-Cevimeline hydrochloride hemihydrate Cat. No.: HY-76772A Cat. No.: HY-76772B

Bioactivity: Cevimeline hydrochloride hemihydrate, a novel muscarinic Bioactivity: Cevimeline hydrochloride hemihydrate, a novel muscarinic receptor agonist, is a candidate therapeutic drug for receptor agonist, is a candidate therapeutic drug for in Sjogren's syndrome. IC50 value: Target: mAChR xerostomia in Sjogren's syndrome. IC50 value: Target: mAChR The general pharmacol. properties of this drug on the The general pharmacol. properties of this drug on the gastrointestinal, urinary, and reproductive systems and other… gastrointestinal, urinary, and reproductive systems and other… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg 1 mg, 5 mg

AC260584 Cat. No.: HY-100336 (LAS 34273; LAS-W 330) Cat. No.: HY-14144

Bioactivity: AC260584 is an M1 muscarinic receptor allosteric agonist Bioactivity: Aclidinium Bromide(LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist as a maintenance treatment for with a pEC50 of 7.6. chronic obstructive pulmonary disease (COPD).

Purity: 98.02% Purity: 99.54% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Alvameline (Lu 25-109) Cat. No.: HY-101586 (BL700) Cat. No.: HY-U00067

Bioactivity: (Lu25-109) is a partial M1 agonist and M2/M3 Bioactivity: Ambutonium bromide is an acetylcholine antagonist. antagonist.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

Anisodamine hydrobromide (6-Hydroxyhyoscyamine) Cat. No.: HY-N0584 (Arecoline bromide) Cat. No.: HY-B0489

Bioactivity: is an anticholinergic and α1-adrenergic receptor Bioactivity: Arecoline Hydrobromide is a muscarinic acetylcholine receptor antagonist used in the treatment of acute circulatory shock, agonist. is also a naturally occurring alkaloid found in some plants of the family.

Purity: 98.0% Purity: 99.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 500 mg, 1 g

Atropine Atropine methyl bromide (Tropine tropate; DL-) Cat. No.: HY-B1205 ( bromide) Cat. No.: HY-112076

Bioactivity: Atropine is a medication used to treat certain types of nerve Bioactivity: Atropine methyl bromide, a muscarinic receptor (mAChR) agent and poisonings, some types of slow heart rate, antagonist, is a quaternary ammonium salt of atropine and a and to decrease saliva production during surgery. mydriatic for dilation of the pupil during ophthalmic examination. It is introduced for relieving pyloric spasm in infants for its highly polar nature. It penetrates less… Purity: 99.55% Purity: 95.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 10 mg, 50 mg, 100 mg

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Atropine sulfate Atropine sulfate monohydrate (Sulfatropinol) Cat. No.: HY-B1205A (Atropine sulfate hydrate) Cat. No.: HY-B0394

Bioactivity: Atropine sulfate is a competitive muscarinic acetylcholine Bioactivity: Atropine sulfate monohydrate is a competitive muscarinic receptor antagonist. acetylcholine receptor antagonist. Target: mAChR Atropine is a naturally occurring tropane alkaloid extracted from deadly nightshade (), Jimson weed ( stramonium), mandrake ( officinarum) and other… Purity: >98% Purity: 99.62% Clinical Data: Launched Clinical Data: Launched Size: 100 mg Size: 10mM x 1mL in DMSO, 100 mg

Batefenterol Benzamide Derivative 1 (GSK961081; TD-5959) Cat. No.: HY-12980 Cat. No.: HY-U00415

Bioactivity: Batefenterol (GSK961081;TD-5959) is a novel muscarinic Bioactivity: Benzamide Derivative 1 is a benzamide derivative from patent EP0213775A1, compound 18. Benzamide Derivative 1 may be useful receptor antagonist and β2-adrenoceptor agonist; displays in treatment of gastrointestinal disorders. high affinity for hM2, hM3 muscarinic and hβ 2-adrenoceptor

with Ki values of 1.4, 1.3 and 3.7 nM, respectively. Purity: 98.30% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 5 mg, 10 mg, 50 mg, 100 mg

Benzetimide hydrochloride Benztropine mesylate ( mesylate; Benzotropine (R4929) Cat. No.: HY-B1547A mesylate; Benztropine methanesulfonate) Cat. No.: HY-B0520A

Bioactivity: Benzetimide hydrochloride is a muscarinic acetylcholine Bioactivity: Benzotropine is a centrally-acting, antimuscarinic agent used receptor antagonist. as an adjunct in the treatment of Parkinson's disease. Target: mAChR Benzotropine is a centrally-acting, antimuscarinic agent used as an adjunct in the treatment of Parkinson's disease. It may also be used to treat extrapyramidal reactions, such as… Purity: 99.44% Purity: 99.86% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 10 mg, 50 mg 1 g

Beperidium iodide (SX 810) Cat. No.: HY-100152 (Carbamyl-β-methylcholine) Cat. No.: HY-B0406

Bioactivity: Beperidium iodide shows a competitive antagonistic effect Bioactivity: Bethanechol is a parasympathomimetic choline carbamate that against acetylcholine receptor with a pA2 of 7.93. selectively stimulates muscarinic receptors without any effect on nicotinic receptors. Target: muscarinic receptor concentration dependently reduced muscle contractions, calcium mobilization, and epithelial secretion… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg Size: 1 g

Bethanechol chloride (Carbamyl-β-methylcholine chloride) Cat. No.: HY-B0406A (KL 373) Cat. No.: HY-13204A

Bioactivity: Bethanechol Chloride is a selective muscarinic receptor Bioactivity: Biperiden(KL 373) is an antiparkinsonian agent, which is the agonist without any effect on nicotinic receptors. selective central M1 cholinoreceptors blocker. Target: M1 receptors Biperiden is an antiparkinsonian agent of the anticholinergic type. It is used for the adjunctive treatment of all forms of Parkinson's disease (postencephalitic,… Purity: 95.00% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 100 mg, 500 mg 200 mg, 5 g

102 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Biperiden Hydrochloride BQCA (KL 373 (Hydrochloride)) Cat. No.: HY-13204 Cat. No.: HY-101858

Bioactivity: Biperiden Hydrochloride (KL 373 Hydrochloride) is an Bioactivity: BQCA a highly selective allosteric modulator of the M1 antiparkinsonian agent, which is the selective central M1 mAChR. cholinoreceptors blocker. Target: M1 receptors Biperiden is an antiparkinsonian agent of the anticholinergic type. It is used for the adjunctive treatment of all forms of Parkinson's… Purity: 98.0% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

BTM-1086 Camylofine Cat. No.: HY-U00406 Cat. No.: HY-B1230

Bioactivity: BTM-1086 is a potent anti-ulcer and gastric secretory Bioactivity: is an antimuscarinic, is a smooth muscle relaxant. inhibiting agent.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 g

Carbamoylcholine chloride CDD0102 (; Carbamylcholine chloride) Cat. No.: HY-B1208 (CDD0102A) Cat. No.: HY-U00230

Bioactivity: Carbamoylcholine chloride is used to study responses mediated Bioactivity: CDD0102 is a potent M1 Muscarinic receptor agonist. by nAChR and mAChR, including smooth muscle contraction, gut motility, and neuronal signaling. IC50 value: 10 to 10,000 nM (Ki) Target: nAChR, mAChR Carbamoylcholine is an analog of acetylcholine that activates acetylcholine receptors (AChR).… Purity: 98.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 100 mg

Cevimeline Cevimeline hydrochloride (AF-102B) Cat. No.: HY-70020 (AF-102B hydrochloride; SNI-2011 hydrochloride) Cat. No.: HY-70020B

Bioactivity: Cevimeline (AF-102B) is a parasympathomimetic and muscarinic Bioactivity: Cevimeline (Evoxac) Hcl is a parasympathomimetic and agonist, with particular effect on M3 receptors; used in the , with particular effect on M3 receptors; treatment of dry mouth associated with sjogren's syndrome. used in the treatment of dry mouth associated with sjogren's syndrome.

Purity: 90.0% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg

Cevimeline hydrochloride hemihydrate CHF5407 Cat. No.: HY-76772 Cat. No.: HY-U00302

Bioactivity: Cevimeline hydrochloride hemihydrate, a novel muscarinic Bioactivity: CHF5407 is a muscarinic M3-receptor antagonist extracted receptor agonist, is a candidate therapeutic drug for from patent WO 2008012290 A2, formula Ic. xerostomia in Sjogren's syndrome.

Purity: 98.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 100 mg, 250 mg, 500 mg 5 mg, 10 mg, 50 mg

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Cimetropium Bromide (DA-3177) Cat. No.: HY-U00106 (Ro 2-3773) Cat. No.: HY-B1132

Bioactivity: (DA-3177) is a mAChR antagonist for Bioactivity: Clidinium bromide is an anticholinergic (specifically a long-term treatment of irritable bowel syndrome. muscarinic antagonist) drug, may help symptoms of cramping and abdominal/stomach pain by decreasing stomach acid, and slowing the intestines.

Purity: 95.34% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg 1 mg, 5 mg, 10 mg, 20 mg

Cyclodrine hydrochloride Darenzepine Cat. No.: HY-U00139 Cat. No.: HY-100154

Bioactivity: Cyclodrine hydrochloride is a cholinergic (muscarinic, Bioactivity: Darenzepine is a muscarinic receptor inhibitor extracted nicotinic) ( mAChR and nAChR) receptor antagonist. from patent US 20170095465 A1.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg

Darifenacin hydrobromide (UK-88525) Cat. No.: HY-A0033 (UK-88525 (hydrobromide)) Cat. No.: HY-A0012

Bioactivity: Darifenacin(UK88525) is a selective M3 muscarinic receptor Bioactivity: Darifenacin hydrobromide is a selective M3 muscarinic receptor antagonist with pKi of 8.9. IC50 value: 8.9 (pKi) [1] Target: antagonist with pKi of 8.9. IC50 value: 8.9 (pKi) [1] Target: M3 receptor in vitro: Darifenacin exerts non-parallel M3 receptor in vitro: Darifenacin exerts non-parallel rightward displacement of the agonist curve and also rightward displacement of the agonist curve and also significant depression of the maximum response… significant depression of the maximum response… Purity: 97.38% Purity: 95.14% Clinical Data: Launched Clinical Data: Launched Size: 10 mg Size: 10mM x 1mL in DMSO, 10 mg, 100 mg

Desfesoterodine Diphenidol hydrochloride (PNU-200577; (R)-5-Hydroxymethyl ) Cat. No.: HY-76569 (Difenidol hydrochloride) Cat. No.: HY-A0082

Bioactivity: (PNU-200577; Desfesoterodine) is a potent and Bioactivity: Diphenidol hydrochloride is a muscarinic antagonist employed selective muscarinic receptor antagonist with a Kb and a pA2 as an antiemetic and as an antivertigo agent. of 0.84 nM and 9.14, respectively.

Purity: 99.66% Purity: 99.60% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 100 mg

Diphenmanil methylsulfate DREADD agonist 21 (Diphemanil mesylate) Cat. No.: HY-16171 Cat. No.: HY-100234

Bioactivity: Diphemanil methylsulfate is a quaternary ammonium Bioactivity: DREADD agonist 21 is a potent human muscarinic acetylcholine

anticholinergic. It binds muscarinic acetycholine receptors M3 receptors ( hM3Dq) agonist( EC50=1.7 nM). and thereby decreases secretory of stomach acids as well as saliva and sweat. IC50 value: Target: mAChR Diphemanil Methylsulfate exerts its action by primarily binding the… Purity: 99.83% Purity: 98.00% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 2 mg, 5 mg, 10 mg

104 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Dronedarone Elucaine (SR 33589) Cat. No.: HY-A0016 Cat. No.: HY-101743

Bioactivity: (SR 33589) is a newer therapeutic agent with a Bioactivity: Elucaine is a muscarinic acetylcholine receptor antagonist structural resemblance to and a better with anti-ulcerative activity. profile; it is a multichannel blocker with antiadrenergic properties and has been evaluated in both rate and rhythm control strategies in the management of AF. Purity: 99.49% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 10 mg, 50 mg

ENS-163 phosphate (ENS 213-163; Sandoz ENS 163 phosphate; fumarate Thiopilocarpine phosphate) Cat. No.: HY-U00038 Cat. No.: HY-A0030

Bioactivity: ENS-163 phosphate is a selective muscarinic M1 receptor Bioactivity: Fesoterodine Fumarate is an antimuscarinic agent and is agonist. rapidly de-esterified to its active metabolite 5-hydroxymethyl tolterodine that is a muscarinic receptor antagonist. IC50 value: Target: mAChR Fesoterodine has the advantage of allowing more flexible dosage than other muscarinic… Purity: >98% Purity: 99.52% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 500 mg

Flavoxate hydrochloride (Rec-7-0040; DW61) Cat. No.: HY-B0549A Cat. No.: HY-B0416

Bioactivity: Hydrochloride(DW-61 Hydrochloride) is a muscarinic Bioactivity: Gallamine Triethiodide is a synthetic nondepolarizing blocking AChR antagonist used in various urinary syndromes and as an drug. .

Purity: 99.0% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in Water, 100 mg, 1 g 100 mg, 500 mg

Glycopyrrolate Bromide (Glycopyrrolate bromide; ) Cat. No.: HY-17465 (Homatropine hydrobromide) Cat. No.: HY-B0547A

Bioactivity: Glycopyrrolate(Glycopyrronium Br) is a muscarinic competitive Bioactivity: Homatropine Bromide is muscarinic AChR antagonist that is an antagonist used as an antispasmodic. anticholinergic medication.

Purity: 98.0% Purity: 99.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 1 g, 5 g

Homatropine methylbromide (Homatropine methobromide) Cat. No.: HY-B1388 (KRP-197; ONO-8025) Cat. No.: HY-B0662

Bioactivity: Homatropine Methylbromide is muscarinic AChR antagonist, Bioactivity: Imidafenacin(KRP-197; ONO-8025) is a potent and selective inhibits endothelial and smooth muscle muscarinic receptors of inhibitor of M3 receptors with Kb of 0.317 nM; less potent for WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, M2 receptors(IC50=4.13 nM). respectively.

Purity: 98.0% Purity: 98.38% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 200 mg, 500 mg 200 mg, 500 mg

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Ipratropium bromide Irsogladine (Sch 1000) Cat. No.: HY-B0241 (Dicloguamine) Cat. No.: HY-B0327

Bioactivity: is a muscarinic antagonist, Bioactivity: Irsogladine is a PDE4 inhibitor and muscarinic acetylcholine bronchodilator, N-Isopropyl salt of atropine. receptor binder.

Purity: 98.0% Purity: 95.13% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 100 mg, 500 mg

Irsogladine maleate L-Hyoscyamine (Dicloguamine maleate; MN1695) Cat. No.: HY-B0327A (Daturine) Cat. No.: HY-N0471

Bioactivity: Irsogladine is a PDE4 inhibitor and muscarinic acetylcholine Bioactivity: L-Hyoscyamine is a chemical compound, a tropane alkaloid it is receptor binder. the levo-isomer to atropine.

Purity: >98% Purity: 99.08% Clinical Data: Launched Clinical Data: No Development Reported Size: 100 mg, 500 mg Size: 10mM x 1mL in DMSO, 100 mg, 500 mg

Levetiracetam LY2119620 (UCB L059) Cat. No.: HY-B0106 Cat. No.: HY-15885

Bioactivity: (UCB L059) is a selective M2 muscarinic Bioactivity: LY2119620 is a high-affinity muscarinic M2/M4 receptor [1] acetylcholine receptors ( mAChR) inhibitor . agonist. Antiepileptic agent [1].

Purity: 99.99% Purity: 99.74% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 500 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

mAChR-IN-1 mAChR-IN-1 hydrochloride Cat. No.: HY-12426 Cat. No.: HY-12426A

Bioactivity: mAChR-IN-1 is a potent muscarinic cholinergic receptor(mAChR) Bioactivity: mAChR-IN-1 hydrochloride is a potent muscarinic cholinergic antagonist with IC50 of 17 nM. [1] receptor (mAChR) antagonist, with an IC50 of 17 nM .

Purity: 99.78% Purity: 99.94% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

Methacholine chloride Methscopolamine bromide (Acetyl-β-methylcholine chloride) Cat. No.: HY-A0083 ((-)-Scopolamine methyl bromide; Hyoscine methyl bromide) Cat. No.: HY-B0344

Bioactivity: chloride is a synthetic choline ester that acts Bioactivity: Methscopolamine (Pamine) is a muscarinic acetylcholine as a non-selective muscarinic receptor agonist in the receptor blocker. Target: mAChR Methylscopolamine is an oral parasympathetic nervous system. medication used along with other medications to treat peptic ulcers by reducing stomach acid secretion. With the advent of proton pump inhibitors and antihistamine medications it is… Purity: 98.0% Purity: 99.44% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 100 mg, 500 mg

106 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Methylbenactyzium Bromide hydrochloride Cat. No.: HY-B2070 Cat. No.: HY-120081B

Bioactivity: Methylbenactyzium Bromide is a muscarinic acetylcholine Bioactivity: Metixene hydrochloride is an anticholinergic antiparkinsonian receptor ( mAChR) inhibitor. agent, potently inhibits binding of quinuclidinyl benzilate (QNB) to the muscarinic receptor in rat brain cortical [1] tissue, with an IC50 of 55 nM and a Kd of 15 nM . Purity: 98.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 50 mg, 100 mg, 200 mg

Metixene hydrochloride hydrate MHP 133 Cat. No.: HY-120081A Cat. No.: HY-101653

Bioactivity: Metixene hydrochloride hydrate is an anticholinergic Bioactivity: MHP 133 is a drug with multiple CNS targets, and inhibits

antiparkinsonian agent, potently inhibits binding of acetylcholinesterase (AChE) with Ki of 69 μM; also active quinuclidinyl benzilate (QNB) to the muscarinic receptor against muscarinic M1 and M2 receptors, serotonin 5HT4 in rat brain cortical tissue, with an IC50 of 55 nM and a Kd<… receptors, and imidazole I2 receptors.

Purity: 99.85% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 10 mg

MK-7622 Nuvenzepine (M1 receptor modulator) Cat. No.: HY-15618 Cat. No.: HY-U00119

Bioactivity: MK-7622 is a muscarinic M1 receptor positive allosteric Bioactivity: Nuvenzepine is an mAChR antagonist previously in phase I modulator. Target: M1 receptor MK-7622 is useful in the clinical trials for the treatment of gastrospasm. treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. Purity: 98.37% Purity: 99.0% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 50 mg, 100 mg

Otilonium bromide (Octylonium bromide; SP63) Cat. No.: HY-B0499A Cat. No.: HY-U00105

Bioactivity: is an antimuscarinic used as a spasmolytic Bioactivity: Oxitropium bromide is an mAChR antagonist used as an agent. anticholinergic bronchodilator drug for the treatment of asthma and chronic obstructive pulmonary disease.

Purity: 95.07% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 5 mg 10 mg, 50 mg

Oxybutynin chloride Cat. No.: HY-B0267 Cat. No.: HY-B0267A

Bioactivity: Oxybutynin is an anticholinergic medication used to relieve Bioactivity: Oxybutynin is an anticholinergic medication used to relieve urinary and bladder difficulties. urinary and bladder difficulties.

Purity: 98.96% Purity: 98.24% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 100 mg, 500 mg

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Pilocarpine Hydrochloride nitrate Cat. No.: HY-B0726 Cat. No.: HY-B1006

Bioactivity: Pilocarpine Hydrochloride is a selective M3-type muscarinic Bioactivity: Pilocarpine nitrate is a selective M3-type muscarinic acetylcholine receptor ( M3 muscarinic receptor) agonist. acetylcholine receptor ( M3 muscarinic receptor) agonist.

Purity: 99.92% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 100 mg, 500 mg Size: 100 mg

Pimethixene Pimethixene maleate (Pimetixene) Cat. No.: HY-B1101 (Pimetixene maleate) Cat. No.: HY-B1101A

Bioactivity: Pimethixene is antihistamine and antiserotonergic compound, Bioactivity: Pimethixene maleate is antihistamine and antiserotonergic acts as an antimigraine agent. Pimethixene is a highly potent compound, acts as an antimigraine agent. Pimethixene maleate

antagonist of 5-HT 1A, 5-HT 2A, 5-HT 2B, 5-HT 2C, is a highly potent antagonist of 5-HT 1A, 5-HT 2A, 5-HT 2B,

histamine H 1, dopamine D 2 and D 4.4 as well as muscari… 5-HT 2C, histamine H 1, dopamine D 2 and D 4.4 as well… Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mg Size: 10 mg

Piperidolate hydrochloride Cat. No.: HY-B0962A Cat. No.: HY-B0962

Bioactivity: Piperidolate is an antimuscarinic, inhibits intestinal cramp Bioactivity: Piperidolate hydrochloride is an antimuscarinic, inhibits induced by acetylcholine (rats and dogs). intestinal cramp induced by acetylcholine (rats and dogs).

Purity: 99.09% Purity: 99.94% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 200 mg 100 mg, 200 mg

Pirenzepine dihydrochloride Pirmenol hydrochloride (LS519) Cat. No.: HY-17037 (Cl-845; (±)-Pirmenol hydrochlorid) Cat. No.: HY-100795A

Bioactivity: dihydrochloride (LS519) is a selective M1 Bioactivity: Pirmenol hydrochloride inhibits IK.ACh by blocking muscarinic receptor antagonist. muscarinic receptors. The IC50 of Pirmenol for inhibition

of Carbachol-induced I K.ACh is 0.1 μM.

Purity: 99.65% Purity: 97.20% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Propantheline bromide Cat. No.: HY-B1188 (Org 9487) Cat. No.: HY-16423

Bioactivity: is an antimuscarinic agent, used for the Bioactivity: Rapacuronium bromide is an allosteric modulator of muscarinic treatment of hyperhidrosis, cramps or spasms of the stomach, acetylcholine receptor ( mAChR). intestines or bladder, and enuresis.

Purity: 95.0% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

108 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Revefenacin Rispenzepine (TD-4208; GSK1160724) Cat. No.: HY-15851 Cat. No.: HY-U00030

Bioactivity: (TD-4208; GSK1160724) is a potent mAChR Bioactivity: Rispenzepine is a novel antimuscarinic compound with a preferential action at M , and M receptor subtypes. antagonist; has a high affinity on M3 receptor with a Ki of 1 3 0.18 nM.

Purity: 99.62% Purity: >98% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

Scopolamine Scopolamine butylbromide (Hyoscine butylbromide; (Hyoscine; Scopine (-)-tropate; Scopine tropate) Cat. No.: HY-N0296 (-)-Scopolamine butylbromide; Butylscopolamine bromide) Cat. No.: HY-N0340

Bioactivity: Scopolamine is a high affinity (nM) muscarinic antagonist. Bioactivity: Scopolamine butylbromide is a competitive antagonist of muscarinic acetylcholine receptor (mAChR) with an IC50 of 55.3 5-HT3 receptor-responses are reversibly inhibited by Scopolamine with an IC of 2.09 μM. ± 4.3 nM. Target: mAChR Scopolamine (USAN), also known as 50 levo-duboisine and hyoscine, sold as Scopoderm, is a tropane alkaloid drug with muscarinic antagonist effects. It is among… Purity: >98% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 100 mg Size: 10mM x 1mL in DMSO, 100 mg, 500 mg

Scopolamine hydrobromide ((-)-Scopolamine hydrobromide; Scopolamine N-oxide hydrobromide Hyoscine hydrobromide; Scopine hydrobromide) Cat. No.: HY-N0296A (Hyoscine N-oxide hydrobromide) Cat. No.: HY-B2146

Bioactivity: Scopolamine hydrobromide is a high affinity (nM) muscarinic Bioactivity: Scopolamine N-oxide hydrobromide is an antagonist of the muscarinic acetylcholine. antagonist. 5-HT3 receptor-responses are reversibly

inhibited by Scopolamine with an IC50 of 2.09 μM.

Purity: 98.0% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 100 mg

Solifenacin hydrochloride (YM905 (free base)) Cat. No.: HY-A0034 (YM905 hydrochloride) Cat. No.: HY-I0230

Bioactivity: Solifenacin (YM905 free base) is a novel muscarinic Bioactivity: Solifenacin Hcl(YM905 Hcl; Vesicare Hcl) is a muscarinic receptor antagonist. receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1,

M2 and M3 receptors, respectively.

Purity: 99.77% Purity: 99.22% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Solifenacin Succinate TAK-071 (YM905) Cat. No.: HY-A0002 Cat. No.: HY-122190

Bioactivity: Solifenacin Succinate(YM905; Vesicare) is a muscarinic Bioactivity: TAK-071 is a novel, potent and highly selective muscarinic receptor antagonist. IC50 value: Target: muscarinic receptor acetylcholine receptor 1 (M1R) positive allosteric Solifenacin succinate (YM905; Vesicare) is a prescription modulator. EC50 of TAK-071 M1R agonist activities is 520 nM medication used to treat certain bladder problems. [1]. Purity: 99.99% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 250 mg, 500 mg 10 mg, 50 mg, 100 mg

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Tarafenacin Tarafenacin D-tartrate (SVT-40776) Cat. No.: HY-14825 (SVT-40776 D-tartrate) Cat. No.: HY-14825A

Bioactivity: Tarafenacin(SVT-40776) is a highly selective M3 muscarinic Bioactivity: Tarafenacin(SVT-40776) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor. M2 receptor.

Purity: >98% Purity: 99.70% Clinical Data: Phase 2 Clinical Data: Phase 2 Size: 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg

TBPB Tematropium Cat. No.: HY-14562 (CDDD3602; HGP6) Cat. No.: HY-U00203

Bioactivity: TBPB is an allosteric M1 mAChR agonist(EC50=289 nM) that Bioactivity: Tematropium (CDDD3602) is a soft . regulates amyloid processing and produces antipsychotic-like activity in rats.

Purity: 99.92% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 50 mg

Temiverine hydrochloride Cat. No.: HY-U00055 (Sesden; SA504) Cat. No.: HY-U00184

Bioactivity: Temiverine hydrochloride is a synthesized drug that is Bioactivity: Timepidium bromide (Sesden; SA504) is an anticholinergic expected to have anticholinergic action. agent.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

Tiotropium Bromide hydrate (BA679 BR) Cat. No.: HY-17360 (BA-679 BR hydrate) Cat. No.: HY-B0460

Bioactivity: Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine Bioactivity: Tiotropium Bromide hydrate is an anticholinergic and receptor (mAChR) antagonist that blocks the binding of the bronchodilator and a muscarinic receptor antagonist. Target: acetylcholine ligand and subsequent opening of the mAChR Tiotropium bromide (Ba 679 BR) is a novel potent and ligand-gated ion channel. long-lasting muscarinic antagonist that has been developed for the treatment of chronic obstructive airways disease (COPD).… Purity: 99.61% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

Tolterodine ((R)-(+)-Tolterodine; (+)-Tolterodine; Tolterodine tartrate (R)-Tolterodine; PNU-200583) Cat. No.: HY-A0024 (Kabi-2234; PNU-200583E) Cat. No.: HY-90010

Bioactivity: Tolterodine(PNU-200583) is a potent muscarinic receptor Bioactivity: Tolterodine Tartrate(PNU-200583E; Kabi-2234) is a potent antagonists that show selectivity for the urinary bladder over muscarinic receptor antagonists that show selectivity for the salivary glands in vivo. urinary bladder over salivary glands in vivo. IC50 Value: Target: mAChR in vitro: Carbachol-induced contractions of isolated guinea pig bladder were effectively inhibited by… Purity: 95.0% Purity: 99.57% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 10 mg, 25 mg, 50 mg, 100 mg, 250 mg

110 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Trihexyphenidyl hydrochloride Cat. No.: HY-B1277 (Ro 1-7683) Cat. No.: HY-B0321

Bioactivity: hydrochloride is an antiparkinsonian agent of Bioactivity: Tropicamide is an anticholinergic and a muscarinic receptor the antimuscarinic class, binds to the M1 muscarinic receptor. subtype M4-preferring antagonist .

Purity: 99.43% Purity: 99.06% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g 100 mg, 500 mg

Trospium chloride Cat. No.: HY-B0461 (GSK573719A) Cat. No.: HY-12100

Bioactivity: is a competitive muscarinic cholinergic Bioactivity: Umeclidinium bromide is a novel mAChR antagonist. The receptor antagonist. affinity ( Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.

Purity: 99.14% Purity: 99.72% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Vinconate VU 0238429 (Chanodesethylapovinc​amine) Cat. No.: HY-U00316 Cat. No.: HY-12157

Bioactivity: Vinconate is an indolonaphthyridine derivative and can Bioactivity: VU 0238429 is positive allosteric modulator of muscarinic stimulate the muscariic acetylcholine receptor. acetylcholine receptor subtype 5 (mAChR5 or M5), with an

EC50 of 1.16 μM.

Purity: >98% Purity: 99.96% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

VU 0365114 VU0152100 Cat. No.: HY-107651 (VU152100) Cat. No.: HY-13340

Bioactivity: VU 0365114 is a mAChR M5 positive allosteric modulator, Bioactivity: VU0152100 is a potent and selective allosteric potentiator of M4 mAChR with an EC50 of 380 ± 93 nM. with an EC50 of 2.7 μM.

Purity: 99.41% Purity: 99.94% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 10 mg, 50 mg

VU0357017 hydrochloride VU0467154 (CID-25010775) Cat. No.: HY-19752A Cat. No.: HY-112209

Bioactivity: VU0357017 hydrochloride is a highly selective M1 agonists that Bioactivity: VU0467154 is a positive allosteric modulator of the M4 appear to act at an allosteric site to activate the receptor muscarinic acetylcholine receptor (mAChR), potentiating the (EC50 = 477 ± 172 nM; pEC50 = 6.37 ± 0.15). IC50 value: 477 ± response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, 172 nM (EC50) [1] Target: M1 in vitro: VU0357017 is a human and cynomolgus monkey M4 receptor, respectively. M1-selective agonists that appear to activate M1 through… Purity: 99.95% Purity: 98.78% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

www.MedChemExpress.com 111

VU6005806 oxalate (AZN-00016130) Cat. No.: HY-128584 (LY246708) Cat. No.: HY-13410

Bioactivity: VU6005806 (AZN-00016130) is a potent muscarnic acethylcholine Bioactivity: Xanomeline oxalate (LY246708) is a selective M1 muscarinic

receptor subtype 4 (M 4) positive allosteric modulator (PAM), receptor agonist. IC50 value: Target: M1 muscarinic receptor with EC s of 94 nM, 28 nM, 87 nM and 68 nM for human, rat, in vitro: Xanomeline had high affinity for muscarinic 50 receptors in brain homogenates, but had substantially less or dog and cyno M , respectively. Used in the research… 4 no affinity for a number of other neurotransmitter receptors… Purity: >98% Purity: 98.87% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

YM-46303 YM-58790 Cat. No.: HY-U00104 Cat. No.: HY-101679

Bioactivity: YM-46303 is an mAChR antagonist which exhibits the highest Bioactivity: YM-58790 is a potent antagonist of M3 muscarinic receptor,

affinities for M1 and M3 receptors, and selectivity for M3 with Ki of 15 nM. over M2 receptor.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

112 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] MC Receptor

Melanocortin receptors (MCRs) comprise a family of five, class A, G protein-coupled receptors designated MC1R-MC5R with diverse physiological roles. MCRs are found in chordates and are regarded as having evolved from a single ancestral receptor, possibly corresponding most closely to MC4R. Signaling by MCRs has primarily been observed as occurring through the stimulatory α unit Gs which activates to produce cAMP. The central nervous melanocortin system is involved in energy homeostasis, regulating food intake and energy expenditure. The brain melanocortin system is defined as the primary neurons that express neuropeptide ligands, and secondary neurons expressing the predominant neural melanocortin receptors (MC3R, MC4R). Mutations in the gene encoding melanocortin receptor agonists, or the genes encoding MC3R or MC4R cause obesity. The other members of the melanocortin receptor family are primarily expressed in the periphery, and are involved in regulating pigmentation (MC1R), adrenal gland function (MC2R), immune function (MC1R/MC3R), and sebaceous gland activity (MC5R).

www.MedChemExpress.com 113 Melanocortin Receptor Inhibitors & Modulators

ACTH (1-17) TFA ACTH 1-17 (α1-17-ACTH (TFA)) Cat. No.: HY-P1545A (α1-17-ACTH) Cat. No.: HY-P1545

Bioactivity: ACTH (1-17) TFA, an adrenocorticotropin analogue, is a potent Bioactivity: ACTH (1-17), an adrenocorticotropin analogue, is a potent

human melanocortin 1 (MC1) receptor agonist with a Ki of human melanocortin 1 (MC1) receptor agonist with a Ki of 0.21 nM. 0.21 nM.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg

Adrenocorticotropic Hormone (ACTH) (1-39), rat Adrenocorticotropic Hormone (ACTH) (1-39), rat TFA (ACTH (1-39) (mouse, rat)) Cat. No.: HY-P1477 (ACTH (1-39) (mouse, rat) (TFA)) Cat. No.: HY-P1477A

Bioactivity: Adrenocorticotropic Hormone (ACTH) (1-39), rat is a potent Bioactivity: Adrenocorticotropic Hormone (ACTH) (1-39), rat (TFA) is a melanocortin 2 (MC2) receptor agonist. potent melanocortin 2 (MC2) receptor agonist.

Purity: >98% Purity: 99.25% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500u g, 1 mg, 5 mg Size: 10mM x 1mL in Water, 500u g, 1 mg, 5 mg

Bremelanotide Acetate JNJ-10229570 (PT-141 Acetate) Cat. No.: HY-18678A Cat. No.: HY-107139

Bioactivity: Bremelanotide Acetate is a melanocortin agonist. IC50 value: Bioactivity: JNJ-10229570 is an antagonist of melanocortin receptor 1 Target: melanocortin in vivo: Bremelanotide is a novel drug (MC1R) and melanocortin receptor 5 (MC5R), which candidate for the treatment of male and female sexual inhibits sebaceous gland differentiation and the production of dysfunction. Bremelanotide has shown promise in effectively sebum-specific lipids. JNJ-10229570 inhibits the binding of treating erectile dysfunction (ED) without the cardiovascular… 125I-NDP-α-MSH to cells expressing human MC1R and MC5R,… Purity: 99.97% Purity: 98.0% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

MC-4R Agonist 1 Nonapeptide-1 acetate salt Cat. No.: HY-U00396 (Melanostatine-5 acetate salt) Cat. No.: HY-P0097A

Bioactivity: MC-4R Agonist 1 is an agonist of human melanocortin-4 Bioactivity: Nonapeptide-1 acetate salt, a peptide hormone, is a potent receptor (MC-4R), used in the research of obesity, α-Melanocyte-stimulating hormone (α-MSH) antagonist, with

diabetes, and . an IC50 of 11 nM. Reduces synthesis of melanin and helps decrease skin pigmentation to a substantial degree [1]. Purity: >98% Purity: 99.76% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg

PF-00446687 Cat. No.: HY-10622 (RM-493; BIM-22493; IRC-022493) Cat. No.: HY-19870

Bioactivity: PF-00446687 is a potent, selective melanocortin-4 receptor Bioactivity: Setmelanotide (RM-493;BIM-22493;IRC-022493) is a [1] ( MC4R) agonist with EC50 of 12±1 nM . Pf-446687 is ( MC4R) agonist with an EC50 of brain penetrant [2]. 0.27 nM for human MC4R.

Purity: >98% Purity: 99.35% Clinical Data: No Development Reported Clinical Data: Launched Size: 250 mg, 500 mg Size: 10mM x 1mL in Water, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

114 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

SNT-207707 SNT-207858 Cat. No.: HY-11029 Cat. No.: HY-11030

Bioactivity: SNT-207707 is a selective, potent and orally active Bioactivity: SNT-207858 is a selective and orally available melanocortin

melanocortin MC-4 receptor antagonist with an IC50 of 8 MC-4 receptor antagonist with a 170-fold selectivity . nM (binding) and 5 nM (function) on the MC-4 receptor. MC-3 and a 40-fold selectivity versus MC-5. SNT-207858 has an IC50 of 8 nM (binding) and 5 nM (function) on the MC-4 receptor. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 250 mg, 500 mg

β-Melanocyte Stimulating Hormone (MSH), human β-Melanocyte Stimulating Hormone (MSH), human TFA (Beta-MSH (1-22) (human)) Cat. No.: HY-P1504 (Beta-MSH (1-22) (human) (TFA)) Cat. No.: HY-P1504A

Bioactivity: β-Melanocyte Stimulating Hormone (MSH), human, a 22-residue Bioactivity: β-Melanocyte Stimulating Hormone (MSH), human TFA, a peptide, acts as an endogenous melanocortin-4 receptor ( 22-residue peptide, acts as an endogenous melanocortin-4 MC4-R) agonist [1]. receptor ( MC4-R) agonist [1].

Purity: >98% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg

γ-1-Melanocyte Stimulating Hormone (MSH), amide Cat. No.: HY-P1531

Bioactivity: γ-1-Melanocyte Stimulating Hormone (MSH), amide is a 11-amino acid peptide. γ-1-Melanocyte Stimulating Hormone (MSH) regulates sodium (Na +) balance and blood pressure through activation of the melanocortin receptor 3 ( MC3-R).

Purity: >98% Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg

www.MedChemExpress.com 115

Melatonin Receptor is a G protein-coupled receptor (GPCR) which binds melatonin. Three types of melatonin receptor have been cloned. The MT1 and MT2 receptor subtypes are present in humans and other mammals, while an additional melatonin receptor subtype MT3 has been identified in amphibia and birds. The MT1 subtype's expression in the pars tuberalis of the pituitary gland and suprachiamatic nuclei of the hypothalamus is indicative of melatonin's circadian and reproductive functional involvement. The MT2 subtype's expression in the retina is suggestive of melatonin's effect on the mammalian retina occurring through this receptor. Research suggests that melatonin acts to inhibit the Ca2+-dependent release of dopamine. Melatonin's action in the retina is believed to affect several light-dependent functions, including phagocytosis and photopigment disc shedding.

116 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Melatonin Receptor Inhibitors & Modulators

Melatonin (N-Acetyl-5-methoxytryptamine) Cat. No.: HY-B0075 (TAK-375) Cat. No.: HY-A0014

Bioactivity: Melatonin is a hormone made by the pineal gland that can Bioactivity: Ramelteon is a highly potent and selective melatonin activates melatonin receptor. Melatonin plays a role in receptor agonist with Ki values of 14 and 112 pM for human sleep and possesses important antioxidative and melatonin1 and melatonin2. anti-inflammatory properties.

Purity: 98.95% Purity: 99.92% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 5 mg, 10 mg, 50 mg, 100 mg, 500 mg

Ramelteon metabolite M-II Cat. No.: HY-103005 (BMS-214778; VEC-162) Cat. No.: HY-14803

Bioactivity: Ramelteon metabolite M-II is the major metabolite of Bioactivity: Tasimelteon is a melatonin MT1 and MT2 receptor agonist.

Ramelteon, with IC 50s of 208 pM, 1470 pM for human melatonin

receptors (MT 1 or MT 2). Ramelteon is a selective melatonin agonist. Purity: >98% Purity: 99.58% Clinical Data: No Development Reported Clinical Data: Launched Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 117 Monoamine Oxidase MAO

Monoamine oxidases (MAO) are a family of enzymes that catalyze the oxidation of monoamines. They are found bound to the outer membrane of mitochondria in most cell types in the body. They belong to the protein family of flavin-containing amine oxidoreductases. Monoamine oxidases catalyze the oxidative deamination of monoamines. Oxygen is used to remove an amine group from a molecule, resulting in the corresponding aldehyde and ammonia. Monoamine oxidases contain the covalently bound FAD and are, thus, classified as flavoproteins. Because of the vital role that MAOs play in the inactivation of neurotransmitters, MAO dysfunction is thought to be responsible for a number of psychiatric and neurological disorders. MAO-A inhibitors act as antidepressant and antianxiety agents, whereas MAO-B inhibitors are used alone or in combination to treat Alzheimer’sand Parkinson’s diseases.

118 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Monoamine Oxidase Inhibitors & Modulators

(S)- (S)-Rasagiline mesylate (TVP1022; S-PAI) Cat. No.: HY-14200 (TVP1022 (mesylate); S-PAI mesylate) Cat. No.: HY-14200A

Bioactivity: (S)-Rasagiline (TVP1022) is the S-isomer of rasagiline, which Bioactivity: (S)-Rasagiline (TVP1022) mesylate is the S-isomer of is an anti-Parkinson drug, appears to have the same rasagiline, which is an anti-Parkinson drug, appears to have neuroprotective activity as the R-isomer, but is 1000-fold the same neuroprotective activity as the R-isomer, but is less active as an MAO-B inhibitor. 1000-fold less active as an MAO-B inhibitor.

Purity: 99.60% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 25 mg 5 mg, 10 mg, 25 mg

2614W94 7-Hydroxy-3,4-dihydro-2(1H)-quinolinone Cat. No.: HY-101578 (3,4-Dihydro-7-hydroxy-2(1H)-quinolinone) Cat. No.: HY-W010130

Bioactivity: 2614W94 is a selective, reversible inhibitor of monoamine Bioactivity: 7-​Hydroxy-​3,​4-​dihydro-​2(1H)​-​quinolinone is a weak MAO-A inhibitor, with an IC of 183 μM, and has no effect oxidase-A with a competitive mechanism of inhibition and IC50 50 [1] of 5 nM and Ki of 1.6 nM with serotonin as substrate. on MAO-B .

Purity: >98% Purity: 99.37% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 100 mg

Amitraz (BTS-27419) Cat. No.: HY-B1111 (CGP 11305A) Cat. No.: HY-13339

Bioactivity: is a non-systemic acaricide and insecticide, with Bioactivity: Brofaromine (CGP 11305A) is a monoamine oxidase ( MAO) alpha- activity, interaction with inhibitor with IC50 of 0.2μM for MAO-A. receptors of the central nervous system and inhibition of monoamine oxidases and synthesis.

Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 100 mg

Clorgyline hydrochloride CX-157 Cat. No.: HY-14197A Cat. No.: HY-100178

Bioactivity: Clorgyline hydrochloride is an irreversible and selective Bioactivity: CX-157 is a reversible inhibitor of monoamine oxidase-A ( inhibitor of (MAO-A) that is used in MAO-A) with an EC50 of 19.3ng/mL. scientific research; structurally related to .

Purity: 99.53% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 10 mg, 50 mg, 100 mg

Desmethoxyyangonin (Demethoxyyangonin; 5,6-Dehydrokavain) Cat. No.: HY-N0918 (LIS 630) Cat. No.: HY-B1413

Bioactivity: is one of the six major found Bioactivity: Eprobemide is a non-competitive reversible inhibitor of in the Piper methysticum () plant; reversible inhibitor of monoamine oxidase A. MAO-B.

Purity: 98.0% Purity: 99.63% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 5 mg, 10 mg, 25 mg, 50 mg

www.MedChemExpress.com 119

GSK-LSD1 Dihydrochloride phosphate Cat. No.: HY-100546A Cat. No.: HY-B0886

Bioactivity: GSK-LSD1 Dihydrochloride is a potent, selective and Bioactivity: Iproniazid is a non-selective, irreversible monoamine oxidase irreversible specific demethylase 1 ( LSD1) inhibitor inhibitor (MAOI) of the hydrazine class.

with an IC50 of 16 nM.

Purity: 98.0% Purity: 99.92% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 mg, 10 mg, 25 mg, 50 mg 100 mg

Isatin (Indoline-2,3-dione) Cat. No.: HY-Y0265 Cat. No.: HY-13929

Bioactivity: Isatin (Indoline-2,3-dione) is a potent inhibitor of Bioactivity: Isocarboxazid is a non-selective and irreversible inhibitor of

monoamine oxidase (MAO) with an IC50 of 3 μM. Also binds monoamine oxidase, with an IC50 of 4.8 μM for rat brain [1] to central benzodiazepine receptors (IC 50 against monoamine oxidase in vitro . , 123 μM) [1]. Also acts as an antagonist of b… Purity: 97.0% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 5 mg 100 mg

Lazabemide MAO-B-IN-1 (Ro 19-6327) Cat. No.: HY-14201 Cat. No.: HY-U00343

Bioactivity: (Ro 19-6327) is selective, reversible monoamine Bioactivity: MAO-B-IN-1 is an inhibitor of , used oxidase B (MAO-B) inhibitor (IC50 values are 0.03 and > 100 for the research of neurological diseases. μM for MAO-B and MAO-A respectively).

Purity: 99.71% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 10 mg, 50 mg

MAO-IN-1 Cat. No.: HY-U00015 Cat. No.: HY-B0884

Bioactivity: MAO-IN-1 is a monoamine oxidase B ( MAO B) inhibitor with Bioactivity: Minaprine is a reversible inhibitor of MAO-A; weakly inhibit acetylcholinesterase; an antidepressant for treatment of an IC50 of 20 nM. depression.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 100 mg

Minaprine dihydrochloride Cat. No.: HY-B0884A (Ro111163) Cat. No.: HY-B0534

Bioactivity: Minaprine 2Hcl is a reversible inhibitor of MAO-A; weakly Bioactivity: Moclobemide(Ro111163) is a reversible monoamine oxidase inhibit acetylcholinesterase; an antidepressant for treatment inhibitor (MAOI) selective for isoform A (RIMA) used to treat of depression. major depressive disorder.

Purity: 99.82% Purity: 99.45% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 50 mg, 100 mg

120 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Mofegiline hydrochloride (MDL72974A) Cat. No.: HY-16677A Cat. No.: HY-B1199

Bioactivity: Hcl (MDL72974A) is a potent and selective Bioactivity: Nialamide is a non-selective, irreversible monoamine oxidase enzyme-activated irreversible inhibitor of MAO-B; shows marked inhibitor (MAOI) of the hydrazine class that was used as an selectivity for the B form (IC50 = 680 and 3.6 nM for MAO-A antidepressant. and MAO-B, respectively.

Purity: 97.19% Purity: 95.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 100 mg

Paeonol Pargyline Cat. No.: HY-N0159 Cat. No.: HY-A0091A

Bioactivity: Paeonol is an active extraction from the root of Paeonia Bioactivity: Pargyline is an irreversible non-selective monoamine oxidase

suffruticosa, Paeonol inhibits MAO-A and MAO-B with IC50 (MAO) inhibitor drug (IC50 for MAO-A is 11.52 nM and for MAO-B of 54.6 μM and 42.5 μM, respectively. is 8.2 nM) .

Purity: 99.98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 500 mg 250 mg, 1 g

Pargyline hydrochloride Cat. No.: HY-A0091 Cat. No.: HY-B1018

Bioactivity: Pargyline hydrochloride is an irreversible inhibitor of Bioactivity: Phenelzine is a non-selective and irreversible monoamine monoamine oxidase (MAO) that is used clinically to treat oxidase inhibitor (MAOI), used as an antidepressant and moderate . anxiolytic.

Purity: 99.91% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg, 500 mg 500 mg

Phenelzine sulfate Rasagiline Cat. No.: HY-B1018A (AGN1135; TVP1012) Cat. No.: HY-14605A

Bioactivity: Phenelzine sulfate is a non-selective and irreversible Bioactivity: Rasagiline(AGN1135;TVP1012) is a new MAO-B inhibitor for the monoamine oxidase inhibitor (MAOI), used as an antidepressant treatment of idiopathic Parkinson's disease. Target: Monoamine and anxiolytic. Oxidase (MAO)-B Rasagiline (N-propargyl-1-(R)-aminoindan) is a novel, highly potent irreversible monoamine oxidase (MAO)-B inhibitor, anti-Parkinsonian drug. Rasagiline is effective as… Purity: 98.70% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 50 mg, 100 mg 100 mg, 500 mg, 1 g, 2 g

Rasagiline 13C3 mesylate racemic Rasagiline mesylate (AGN1135 13C3 racemic; TVP1012 13C3 racemic) Cat. No.: HY-14605BS (AGN1135 (mesylate); TVP1012 (mesylate)) Cat. No.: HY-14605

Bioactivity: Rasagiline 13C3 mesylate racemic is the deuterium labeled Bioactivity: Rasagiline Mesylate is a new MAO-B inhibitor for the treatment Rasagiline, which is an irreversible inhibitor of monoamine of idiopathic Parkinson's disease. Target: Monoamine Oxidase oxidase. (MAO)-B Rasagiline (N-propargyl-1-(R)-aminoindan) is a novel, highly potent irreversible monoamine oxidase (MAO)-B inhibitor, anti-Parkinsonian drug. Rasagiline is effective as… Purity: >98% Purity: 97.56% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in Water, 50 mg, 100 mg

www.MedChemExpress.com 121

Ro 41-1049 hydrochloride Cat. No.: HY-100027A (Labiatenic acid) Cat. No.: HY-N0529

Bioactivity: Ro 41-1049 hydrochloride is a selective, reversible, Bioactivity: Rosmarinic acid (RA) is a widespread phenolic ester compound orally-active MAO-A inhibitor. in the plants. Rosmarinic acid inhibits MAO-A, MAO-B and

COMT enzymes with IC50s of 50.1, 184.6 and 26.7 μM, respectively.

Purity: 99.96% Purity: 99.06% Clinical Data: No Development Reported Clinical Data: Phase 4 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 50 mg, 100 mg

Rosmarinic acid racemate RS 8359 Cat. No.: HY-N2336 Cat. No.: HY-14260

Bioactivity: Rosmarinic acid racemate is the racemate of Rosmarinic acid. Bioactivity: RS 8359 is a selective and reversible MAO-A inhibitor, with Rosmarinic acid inhibits MAO-A, MAO-B and COMT antidepressant activity.

enzymes with IC50s of 50.1, 184.6 and 26.7 μM, respectively.

Purity: 98.01% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 50 mg, 100 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

Safinamide Salsolidine (EMD 1195686; FCE 26743) Cat. No.: HY-70057 (6,7-Dimethoxy-1-methyl-1,2,3,4-tetrahydroisoquinoline) Cat. No.: HY-22385

Bioactivity: (EMD 1195686; FCE 26743) selectively and reversibly Bioactivity: Salsolidine is a tetrahydroisoquinoline alkaloid, acts as a inhibits MAO-B with IC50 of 98 nM, exhibits 5918-fold stereoselective competitive MAO A inhibitor. selectivity against MAO-A.

Purity: 99.77% Purity: 95.77% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 25 mg, 50 mg, 100 mg

TB5 Cat. No.: HY-100975 (MD 69276) Cat. No.: HY-14196

Bioactivity: TB5 is a potent, selective and reversible inhibitor of Bioactivity: Toloxatone (MD 69276) is a reversible monoamine oxidase A hMAO-B with a K value of 0.11±0.01 μM. [1] [1] i ( MAOA) inhibitor . Antidepressant .

Purity: 98.0% Purity: 99.34% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Tranylcypromine hemisulfate (dl- hemisulfate; Vafidemstat trans-2-Phenylcyclopropylamine hemisulfate salt) Cat. No.: HY-B1496 (ORY-2001) Cat. No.: HY-112623

Bioactivity: Tranylcypromine hemisulfate is an irreversible, nonselective Bioactivity: Vafidemstat (ORY-2001) is a dual lysine-specific histone MAO inhibitor used in the treatment of depression. demethylase ( LSD1)/ MAO-B inhibitor.

Purity: 99.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 500 mg, 250 mg 100 mg

122 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] nAChR Nicotinic acetylcholine receptors

nAChRs (nicotinic acetylcholine receptors) are receptor proteins that signal for muscular contraction upon a chemical stimulus. They are cholinergic receptors that form ligand-gated ion channels in the plasma membranes of certain neurons and on the presynaptic and postsynaptic sides of theneuromuscular junction. Nicotinic acetylcholine receptors are the best-studied of the ionotropic receptors. Like the other type of acetylcholine receptor-the muscarinic acetylcholine receptor (mAChR)-the nAChR is triggered by the binding of the neurotransmitter acetylcholine (ACh). Just as muscarinic receptors are named such because they are also activated by muscarine, nicotinic receptors can be opened not only by acetylcholine but also by nicotine —hence the name "nicotinic".

www.MedChemExpress.com 123 nAChR Inhibitors & Modulators

(+)- (-)-(S)-B-973B Cat. No.: HY-W008350 Cat. No.: HY-114269

Bioactivity: (+)-Sparteine is a natural alkaloid acting as a ganglionic Bioactivity: (-)-(S)-B-973B is a potent allosteric agonist and positive blocking agent. (+)-Sparteine competitively blocks nicotinic allosteric modulator of α7 nAChR, with antinociceptive ACh receptor in the neurons. activity [1].

Purity: 98.0% Purity: 99.93% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

(±)- A-867744 (CMI 545) Cat. No.: HY-101078 Cat. No.: HY-12149

Bioactivity: (±)-Epibatidine is a . (±)-Epibatidine is a Bioactivity: A-867744 is a positive allosteric modulator of α7 nAChRs (IC50 neuronal nAChR agonist. values are 0.98 and 1.12 μM for human and rat α7 receptor ACh-evoked currents respectively, in X. laevis oocytes). Displays no activity at 5-HT3A, α3β4 or α4β2 nAChRs. IC50 value: ~ 1 uM Target: α7 nAChR Target: Purity: >98% Purity: 99.92% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg

Adiphenine hydrochloride Cat. No.: HY-B0379A ((S)-Anabasine) Cat. No.: HY-B1532

Bioactivity: Adiphenine HCl is a nicotinic receptor inhibitor, used as an Bioactivity: Anabasine is a nicotinic receptor agonist. antispasmodic drug.

Purity: 99.62% Purity: 98.71% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 10 mg, 25 mg, 50 mg, 100 mg

Aniracetam Atracurium besylate (Ro 13-5057) Cat. No.: HY-10932 (BW-33A) Cat. No.: HY-B0292A

Bioactivity: Aniracetam(Ro 13-5057) is a nootropics and neuroprotective Bioactivity: Atracurium Besylate is a neuromuscular blocking agent with drug, which is selectively modulates the AMPA receptor and ED95 of 0.2 mg/kg. Target: nAChR Atracurium besylate is a nAChR. neuromuscular-blocking drug or skeletal muscle relaxant in the category of non-depolarizing neuromuscular-blocking drugs, used adjunctively in anesthesia to facilitate endotracheal… Purity: 99.43% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 50 mg, 100 mg, 500 mg

BNC375 Carbamoylcholine chloride Cat. No.: HY-128575 (Carbachol; Carbamylcholine chloride) Cat. No.: HY-B1208

Bioactivity: BNC375 is a potent, selective, and orally available type I Bioactivity: Carbamoylcholine chloride is used to study responses mediated

positive allosteric modulator of α7 nAChRs with an EC50 of by nAChR and mAChR, including smooth muscle contraction, gut motility, and neuronal signaling. IC50 value: 10 to 10,000 nM 1.9 μM [1]. (Ki) Target: nAChR, mAChR Carbamoylcholine is an analog of acetylcholine that activates acetylcholine receptors (AChR).… Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 250 mg, 100 mg, 500 mg Size: 10mM x 1mL in DMSO, 100 mg

124 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Catharanthine Cholesterol myristate ((+)-3,4-Didehydrocoronaridine) Cat. No.: HY-N0252 (Cholesteryl myristate; Cholesteryl tetradecanoate) Cat. No.: HY-N2338

Bioactivity: Catharanthine inhibits nicotinic receptor mediated diaphragm Bioactivity: Cholesterol myristate is a natural steroid present in contractions with IC50 of 59.6 μM. Target: nAChR Catharanthine traditional Chinese medicine. Cholesterol myristate binds to evokes a concentration-dependent attenuation of carbachol several ion channels such as the nicotinic acetylcholine responses in the rat ileum preparation, producing rightward receptor, GABAA receptor, and the inward-rectifier curve displacements and decreases in maximal agonist… potassium ion channel. Purity: 98.66% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg 50 mg, 100 mg

Cisatracurium besylate Cyclodrine hydrochloride (51W89) Cat. No.: HY-13596 Cat. No.: HY-U00139

Bioactivity: Cisatracurium Besylate (51W89) is a nondepolarizing Bioactivity: Cyclodrine hydrochloride is a cholinergic (muscarinic, neuromuscular blocking agent, antagonizing the action of nicotinic) ( mAChR and nAChR) receptor antagonist. acetylcholine by inhibiting neuromuscular transmission.

Purity: 98.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 1 mg, 5 mg, 10 mg, 20 mg 25 mg, 50 mg, 100 mg

Cytisinicline Bromide (; Sophorine; Baptitoxine) Cat. No.: HY-N0175 Cat. No.: HY-B0570

Bioactivity: Cytisinicline (Cytisine) is an alkaloid that occurs naturally Bioactivity: Decamethonium Bromide is a nicotinic AChR partial agonist and in several plant genera, such as Laburnum and Cytisus. neuromuscular blocking agent. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs [1], and partial to full agonist at β4 containing recept…

Purity: 98.0% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 25 mg 5 g, 10 g

Desformylflustrabromine hydrochloride (Deformylflustrabromine hydrochloride; dFBr hydrochloride) Cat. No.: HY-107675 (MTI-446) Cat. No.: HY-B0827

Bioactivity: hydrochloride is a selective agonist Bioactivity: Dinotefuran is an insecticide of the class, its

of α4β2 neuronal nicotinic acetylcholine receptor ( nAChR) involves disruption of the insect's with a pEC of 6.48. nervous system by inhibiting nicotinic acetylcholine 50 receptors. Target: nAChR, Antiparasitic

Purity: 99.77% Purity: 99.63% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 50 mg, 100 mg

Encenicline hydrochloride (EVP-6124) Cat. No.: HY-15430 (EVP-6124 (hydrochloride)) Cat. No.: HY-15430A

Bioactivity: Encenicline (EVP-6124) is a novel partial agonist of α7 Bioactivity: Encenicline hydrochloride (EVP-6124 hydrochloride) is a novel neuronal nicotinic acetylcholine receptors ( nAChRs). partial agonist of α7 neuronal nicotinic acetylcholine receptors ( nAChRs).

Purity: >98% Purity: 98.20% Clinical Data: Phase 3 Clinical Data: Phase 3 Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 125

GTS-21 dihydrochloride Bromide (DMXB-A; DMBX-anabaseine) Cat. No.: HY-14564A Cat. No.: HY-B0569

Bioactivity: GTS-21 dihydrochloride is a selective α7 nicotinic Bioactivity: Hexamethonium Bromide is a non-depolarising ganglionic acetylcholine receptor agonist, has recently been established blocker, a nicotinic nACh (NN) receptor antagonist. Target: as a promising treatment for inflammation. nAChR Hexamethonium Bromide is a non-depolarising , a nicotinic nACh receptor antagonist that acts in autonomic ganglia by binding mostly in or on the NN receptor,… Purity: 99.76% Purity: 98.0% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 g, 5 g

Lobeline hydrochloride Meclofenoxate hydrochloride (α- hydrochloride; L-Lobeline hydrochloride) Cat. No.: HY-B0979 Cat. No.: HY-17555

Bioactivity: Lobeline hydrochloride, a nicotinic receptor agonist, acting Bioactivity: Meclofenoxate hydrochloride, an ester of dimethylethanolamine as a potent antagonist at both α3β2 and α4β2 neuronal (DMAE) and 4-chlorophenoxyacetic acid (pCPA), has been shown nicotinic receptor subtypes. to improve memory, have a mentally stimulating effect, and improve general cognition.

Purity: 99.97% Purity: 98.32% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in Water, 100 mg, 500 mg 100 mg

Methyllycaconitine citrate Monepantel (MLA) Cat. No.: HY-N2332A (AAD1566) Cat. No.: HY-14774

Bioactivity: citrate is a specific antagonist of α7 Bioactivity: Monepantel is organic anthelmintic, and acts as a positive neuronal nicotinic acetylcholine receptor ( α7nAChR). allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor ( nAChR) subunits.

Purity: 98.0% Purity: 99.43% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

N-Methylcytisine Nelonicline (Caulophylline) Cat. No.: HY-N0443 (ABT-126) Cat. No.: HY-16748

Bioactivity: N-Methylcytisine (Caulophylline), a tricyclic quinolizidine Bioactivity: Nelonicline (ABT-126) is a selective neuronal nicotinic receptor alkaloid, exerts hypoglycaemic, analgesic and agonist. anti-inflammatory activities. N-methylcytisine is a selective ligand of nicotinic receptors of acetylcholine in the central

nervous system and has a high affinity ( Kd = 50 nM) to… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size: 250 mg, 500 mg

NS 1738 Pancuronium dibromide (NSC 213859) Cat. No.: HY-12151 Cat. No.: HY-B0429

Bioactivity: NS 1738 (NSC 213859) is a novel positive allosteric modulator Bioactivity: Pancuronium Dibromide is a bis-quaternary steroid that is a of the α7 nAChR, with respect to positive modulation of α7 competitive . Target: nAChR Pancuronium

nAChR (EC 50=3.4 μM in oocyte experiments). dibromide is a competitive AChR antagonist (IC50 = 5.5 nM) and acts as a skeletal muscle relaxant. Pancuronium dibromide interrupts neuromuscular transmission by competing with… Purity: 99.21% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 mg, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

126 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

PNU-120596 PNU-282987 (NSC 216666) Cat. No.: HY-12152 Cat. No.: HY-12560A

Bioactivity: PNU-120596 (NSC 216666 ) is a potent and selective positive Bioactivity: PNU-282987 is a selective α7 nicotinic acetylcholine allosteric α7 nAChR modulator with an EC50 of 0.2 μM. receptor(α7 nAChR) agonist with Ki of 26 nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM). IC50 value: 26 nM(Ki) [1] Target: α7 nAChR agonist in vitro: Treatment with PNU-282987 resulted in an attenuation of neuroinflammation in… Purity: 98.15% Purity: 99.70% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

PNU-282987 S enantiomer free base Cat. No.: HY-12560D (RJR-2403; (E)-Metanicotine) Cat. No.: HY-13225A

Bioactivity: PNU-282987 S enantiomer free base is the S-enantiomer of Bioactivity: Rivanicline (RJR-2403) is a neuronal nicotinic receptor PNU-282987 free base. PNU-282987 is an α7 nicotinic agonist, showing high selectivity for the α4β2 subtype (Ki=26 acetylcholine receptor (α7 nAChR) agonist. nM); > 1,000 fold selectivity than α7 receptors(Ki= 36000 nM). IC50 value: 26 nM [1] Target: α4β2 nAChR in vitro: At concentrations up to 1 mM, Rivanicline does not significantly… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 2 mg, 5 mg

Rivanicline hemioxalate Rivanicline oxalate (RJR-2403 (hemioxalate); (E)-Metanicotine (hemioxalate)) Cat. No.: HY-13225B (RJR-2403 (oxalate); (E)-Metanicotine (oxalate)) Cat. No.: HY-13225

Bioactivity: Rivanicline hemioxalate (RJR-2403 hemioxalate) is a neuronal Bioactivity: Rivanicline oxalate (RJR-2403 oxalate) is a neuronal nicotinic nicotinic receptor agonist, showing high selectivity for the receptor agonist, showing high selectivity for the α4β2 α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 36000 nM). IC50 value: 26 nM [1] Target: α4β2 receptors(Ki= 36000 nM). nAChR in vitro: At concentrations up to 1 mM, Rivanicline does… Purity: 95.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 10 mg, 50 mg

S16961 Sofiniclin (S169611) Cat. No.: HY-U00281 (ABT 894) Cat. No.: HY-14824

Bioactivity: S16961 is a nicotinic receptor agonist. Bioactivity: Sofiniclin (ABT 894) is an agonist of nicotinic acetylcholine receptor (nAChR), used as a potential non-stimulant treatment for attention-deficit/hyperactivity disorder (ADHD).

Purity: >98% Purity: 95.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

Tebanicline hydrochloride (Ebanicline hydrochloride; ABT-594 hydrochloride) Cat. No.: HY-14316A (CP 526555) Cat. No.: HY-10019

Bioactivity: hydrochloride (ABT594 hydrochloride) is a nAChR Bioactivity: Varenicline (CP 526555) is a selective α4β2 nicotinic receptor modulator with potent, orally effective analgesic activity. It (nAChR) partial agonist. inhibits the binding of cytisine to α4β2 neuronal nAChRs with

a Ki of 37 pM.

Purity: 98.00% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

www.MedChemExpress.com 127

Varenicline Hydrochloride Varenicline Tartrate (CP 526555 hydrochloride) Cat. No.: HY-10020 (CP 526555-18) Cat. No.: HY-10021

Bioactivity: Varenicline Hcl(CP 526555;Champix) is a nicotinic receptor Bioactivity: Varenicline Tartrate(CP 526555;Champix) is a nicotinic partial agonist; it stimulates nicotine receptors more weakly receptor partial agonist; it stimulates nicotine receptors than nicotine itself does. IC50 value: Target: nAChR more weakly than nicotine itself does. IC50 value: Target: Varenicline(CP 526555; Champix; Chantix) is a prescription α4β2 nAChR Varenicline(CP 526555; Champix; Chantix) is a medication used to treat addiction. As a partial… prescription medication used to treat smoking addiction. As a… Purity: >98% Purity: 99.90% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Vecuronium bromide Zaldaride maleate (ORG NC 45) Cat. No.: HY-B0118A (CGS-9343B; KW 5617) Cat. No.: HY-105118A

Bioactivity: is a nondepolarizing neuromuscular blocking Bioactivity: Zaldaride maleate (CGS-9343B) is a potent and selective agent of intermediate duration. inhibitor of calmodulin. Zaldaride maleate (CGS-9343B) inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase [1] [2] activity, with an IC50 of 3.3 nM . Zaldaride maleate (CGS-9343B) prevents -induced transcription activation… Purity: 98.0% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 10 mg, 50 mg, 100 mg 5 mg

ZSET1446 (ST-101) Cat. No.: HY-11013

Bioactivity: ZSET1446 is a novel cognitive enhancer that significantly improves learning deficits in various types of Alzheimer disease (AD) models.

Purity: 98.03% Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

128 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Neurokinin Receptor NK receptor

There are three main classes of neurokinin receptors: NK1R (the preferring receptor), NK2R, and NK3R. These tachykinin receptors belong to the class I (rhodopsin-like) G-protein coupled receptor (GPCR) family. The various tachykinins have different binding affinities to the neurokinin receptors: NK1R, NK2R, and NK3R. These neurokinin receptors are in the superfamily of transmembrane G-protein coupled receptors (GPCR) and contain seven transmembrane loops. Neurokinin-1 receptor interacts with the Gαq-protein and induces activation of phospholipase C followed by production of inositol triphosphate (IP3) leading to elevation of intracellular calcium as a second messenger. Further, cyclic AMP (cAMP) is stimulated by NK1R coupled to the Gαs-protein. The neurokinin receptors are expressed on many cell types and tissues.

www.MedChemExpress.com 129 Neurokinin Receptor Inhibitors & Modulators

Aprepitant (MK-0869; MK-869; L-754030) Cat. No.: HY-10052 (Ro67-5930) Cat. No.: HY-19670

Bioactivity: (MK-0869) is a selective and high-affinity Bioactivity: Befetupitant is a high-affinity, nonpeptide, competitive

neurokinin 1 receptor antagonist with a Kd of 86 pM. tachykinin 1 receptor ( NK1R) antagonist.

Purity: 99.93% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

Fezolinetant (ESN-364) Cat. No.: HY-19632 (L-758298) Cat. No.: HY-14407

Bioactivity: is an antagonist of the neurokinin 3 receptor Bioactivity: Fosaprepitant (L-758298) is a neurokinin-1 receptor antagonist (NK3R), used for the treatment of menopausal hot flushes. for the prevention of chemotherapy-induced nausea and vomiting.

Purity: 98.29% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Fosaprepitant dimeglumine GR 159897 (MK-0517; L785298) Cat. No.: HY-14407A Cat. No.: HY-107691

Bioactivity: Fosaprepitant dimeglumine(MK-0517) is a neurokinin-1 receptor Bioactivity: GR 159897 is a highly potent, selective, competitive,

antagonist for the prevention of chemotherapy-induced nausea brain-penetrated non-peptide antagonist at tachykinin NK2 and vomiting. IC50 Value: Target: NK1 receptor in vitro: receptors, inhibits binding of [ 3H]GR100679 to hNK -CHO Fosaprepitant (also known as MK-0517 and L-758,298) is a 2 water-soluble phosphoryl prodrug for aprepitant, which, when… cells and rat colon membranes with pKis of 9.51 and … Purity: 99.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg Size:

Hemokinin 1 mouse Cat. No.: HY-P1030 (MEN 15596) Cat. No.: HY-14770

Bioactivity: Hemokinin 1 (mouse) is a selective agonist of neurokinin-1 Bioactivity: Ibodutant (MEN 15596) is a potent and selective tachykinin NK2

receptor, with Ki of 0.175 nM and 560 nM for human NK1 receptor antagonist with a pKi of 10.1. receptor and human NK2 receptor, respectively.

Purity: 98.41% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 250 mg, 500 mg

Kassinin Cat. No.: HY-P0250 Cat. No.: HY-10053

Bioactivity: Kassinin is a peptide derived from the Kassina frog. It Bioactivity: Maropitant is a neurokinin (NK1) receptor antagonist. IC50 belongs to tachykinin family of neuropeptides. It is secreted value: Target: NK1 receptor Maropitant is the first NK1 as a defense response, and is involved in neuropeptide receptor antagonist developed to treat and prevent emesis in signalling. dogs. Treatment with 1 mg/kg Maropitant citrate, significantly reduced the size of ulcerative dermatitis (UD) lesions in… Purity: >98% Purity: 99.00% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 25 mg Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 25 mg

130 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Men 10376 Men 10376 TFA (Neurokinin-2 receptor antagonist) Cat. No.: HY-P1276 (Neurokinin-2 receptor antagonist (TFA)) Cat. No.: HY-P1276A

Bioactivity: Men 10376 is a selective tachykinin NK-2 receptor antagonist, Bioactivity: Men 10376 TFA is a selective tachykinin NK-2 receptor

with a Ki of 4.4 μM for rat small intestine NK-2 receptor. antagonist, with a Ki of 4.4 μM for rat small intestine NK-2 receptor [1].

Purity: >98% Purity: 99.76% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg

MEN11467 Monohydroxy D6 Cat. No.: HY-U00207 Cat. No.: HY-G0012S

Bioactivity: MEN11467 is a selective and orally- effective peptidomimetic Bioactivity: Monohydroxy Netupitant D6 is the deuterium labeled Monohydroxy

tachykinin NK1 receptor antagonist. Netupitant, which is a metabolite of Netupitant.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg

Netupitant Netupitant D6 (CID 6451149) Cat. No.: HY-16346 (CID-6451149 D6) Cat. No.: HY-16346S

Bioactivity: Netupitant (CID-6451149) is a highly potent and selective, Bioactivity: Netupitant D6 is the deuterium labeled orally active neurokinin-1 receptor antagonist with Ki of 0.95 Netupitant(CID-6451149), which is a highly potent and nM. IC50 value: 0.95 nM (Ki) [1] Target: NK1 receptor in selective, orally active neurokinin-1 receptor antagonist. vitro: Netupitant also dose-dependently inhibited the SP response as expected from an NK1 receptor antagonist.… Purity: 99.78% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 5 mg, 10 mg, 50 mg, 100 mg

Netupitant metabolite Monohydroxy Netupitant (Monohydroxy Netupitant) Cat. No.: HY-G0012 (α-Neurokinin; Neuromedin L; Substance K) Cat. No.: HY-P0197

Bioactivity: Monohydroxy Netupitant is the metabolite of Netupitant, which Bioactivity: Neurokinin A acts via neurokinin 2 ( NK-2) receptor. is a highly selective NK1 receptor antagonist.

Purity: >98% Purity: 98.92% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg, 25 mg

Neurokinin A(4-10) Neurokinin A(4-10) TFA Cat. No.: HY-P0236 Cat. No.: HY-P0236A

Bioactivity: Neurokinin A (4-10) is a tachykinin NK2 receptor agonist. Bioactivity: Neurokinin A (4-10) TFA is a tachykinin NK2 receptor agonist [1].

Purity: >98% Purity: 98.48% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 25 mg Size: 1 mg, 5 mg, 10 mg, 25 mg

www.MedChemExpress.com 131

Neurokinin antagonist 1 Cat. No.: HY-U00320 Cat. No.: HY-P0242

Bioactivity: Neurokinin antagonist 1 is a Neurokinin antagonist Bioactivity: Neurokinin B belongs to the tachykinin family of peptides. extracted from patent WO1998045262A1. Neurokinin B binds a family of GPCRs-including neurokinin receptor 1 (NK1R), NK2R, and NK3R-to mediate their biological effect [1].

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg, 25 mg

Neurokinin B TFA NK-1 Antagonist 1 Cat. No.: HY-P0242A Cat. No.: HY-106659

Bioactivity: Neurokinin B TFA belongs to the tachykinin family of peptides. Bioactivity: NK-1 Antagonist 1 is an antagonist of NK-1 receptor, used in Neurokinin B binds a family of GPCRs-including neurokinin the research of NK-1 related diseases and conditions such as receptor 1 (NK1R), NK2R, and NK3R-to mediate their biological , overactive bladder, alcohol dependency and depression. effect [1].

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 250 mg, 500 mg 1 mg, 5 mg, 10 mg, 25 mg

NKP608 Pavinetant Cat. No.: HY-18006 (MLE-4901; AZD2624; AZD4901) Cat. No.: HY-14432

Bioactivity: NKP608 is a non-peptidic derivative of 4-aminopiperidine which Bioactivity: Pavinetant (MLE-4901) is a neurokinin-3 receptor ( NK3R) acts as a selective, specific and potent antagonist at the antagonist. neurokinin-1 (NK-1) receptor both in vitro(IC50=2.6 nM) and in vivo.

Purity: 99.34% Purity: 99.74% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Physalaemin Cat. No.: HY-P0255 (SCH619734) Cat. No.: HY-14751

Bioactivity: Physalaemin, a non-mammalian tachykinin, binds selectively to Bioactivity: Rolapitant (SCH619734) is a potent, selective and orally

neurokinin-1 ( NK1) receptor with high affinity. active neurokinin NK1 receptor antagonist with a Ki of 0.66 nM.

Purity: >98% Purity: 98.01% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 25 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Saredutant SB-222200 (SR 48968; SR 48968C) Cat. No.: HY-106910 Cat. No.: HY-15722

Bioactivity: is a selective NK2 receptor antagonist. Bioactivity: SB 222200 is a selective, reversible and competitive antagonist of human NK-3 receptor(Ki=4.4 nM) that effectively crosses the blood-brain barrier.

Purity: >98% Purity: 99.91% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

132 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Scyliorhinin II Senktide Cat. No.: HY-P1588 Cat. No.: HY-P0187

Bioactivity: Scyliorhinin II is a selective neurokinin-3 receptor agonist, Bioactivity: Senktide is a tachykinin NK3 receptor agonist. with a Ki of 2.5 nM for neurokinin-3 receptor in rat cerebral cortex.

Purity: >98% Purity: 99.56% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 25 mg Size: 1 mg, 5 mg, 10 mg, 25 mg

Serlopitant Substance P (VPD-737; MK-0594) Cat. No.: HY-12114 (Neurokinin P) Cat. No.: HY-P0201

Bioactivity: is a selective Neurokinin-1 (NK-1) receptor Bioactivity: Substance P is a neuropeptide, acting as a neurotransmitter antagonist. and as a neuromodulator.The endogenous receptor for substance P is neurokinin 1 receptor ( NK1-receptor, NK1R).

Purity: >98% Purity: 98.07% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 250 mg, 500 mg Size: 1 mg, 5 mg, 10 mg, 25 mg

Substance P (1-7)(TFA) Substance P 1-7 (Substance P (1-7) Trifluoroacetate) Cat. No.: HY-P1485A Cat. No.: HY-P1485

Bioactivity: Substance P (1-7)(TFA) is a fragment of the neuropeptide, Bioactivity: Substance P (7-11) is a fragment of the neuropeptide, substance P (SP). Substance P (1-7)(TFA) gives depressor and substance P (SP). Substance P (7-11) gives depressor and bradycardic effects when applied to the nucleus tractus bradycardic effects when applied to the nucleus tractus solitarius. solitarius.

Purity: 99.20% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 25 mg Size: 5 mg, 10 mg

Substance P 1-9 Substance P 7-11 Cat. No.: HY-P1494 Cat. No.: HY-P1492

Bioactivity: Substance P (1-9) is nonapeptide, which decreases the Bioactivity: Substance P (7-11) is a C-terminal fragment of Substance P inactivation of substance P by the guinea-pig ileum and which can cause an increase in the intracellular calcium urinary bladder. concentration.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 5 mg, 10 mg, 25 mg

Tachykinin angatonist 1 Cat. No.: HY-U00392 (SB 223412) Cat. No.: HY-14552

Bioactivity: Tachykinin angatonist 1 is a neurokinin receptor antagonist Bioactivity: Talnetant (SB 223412) is a potent and selective NK3 receptor extracted from patent US5968923, compound example 32. antagonist(ki=1.4 nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM.

Purity: >98% Purity: 99.44% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

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Talnetant hydrochloride (SB 223412 hydrochloride; SB 223412-A) Cat. No.: HY-14552A (VLY-686; LY686017) Cat. No.: HY-16732

Bioactivity: Talnetant Hcl(SB 223412 Hcl) is a potent and selective NK3 Bioactivity: Tradipitant is a neurokinin-1 ( NK-1) antagonist. receptor antagonist(ki=1.4 nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM.

Purity: >98% Purity: 99.62% Clinical Data: Phase 2 Clinical Data: Phase 2 Size: 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Vofopitant Y1 receptor antagonist 1 (GR 205171) Cat. No.: HY-12142 Cat. No.: HY-101704

Bioactivity: is potent tachykinin NK1 receptor antagonist, with Bioactivity: Y1 receptor antagonist 1, an isomer of H-409/22, is a neuropeptide Y1 receptor antagonist. pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK 1 receptor, respectively.

Purity: >98% Purity: 95.03% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg, 100 mg Size: 1 mg

[bAla8]-Neurokinin A(4-10) [Nle11]-Substance P (MEN 10210) Cat. No.: HY-P1031 Cat. No.: HY-P1506

Bioactivity: [bAla8]-Neurokinin A(4-10) is a neurokinin 2 (NK2) receptor Bioactivity: [Nle11]-Substance P is a substance P analog that avoids agonist. methionine oxidation problems.

Purity: 98.17% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg

[Sar9,Met(O2)11]-Substance P [Sar9] Substance P Cat. No.: HY-P1012 Cat. No.: HY-P1738

Bioactivity: [Sar9,Met(O2)11]-Substance P is a tachykinin NK1 receptor Bioactivity: [Sar9] Substance P is a potent and selective neurokinin (NK)-1 [1] selective agonist. receptor agonist .

Purity: 98.45% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 25 mg Size:

134 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Opioid Receptor

Opioid receptors are a group of G protein-coupled receptors with as ligands. The endogenous opioids are , , endorphins, and . Opioid receptors are distributed widely in the brain, and are found in the spinal cord and digestive tract. Opioid receptors are molecules, or sites, within the body that are activated by opioid substances. Opioid receptors inhibit the transmission of impulse in excitatory pathways within the human body system. These pathways include the serotonin, catecholamine, and substance P pathways, which are all implicated in pain perception and feelings of well-being. Opioid receptors are further subclassified into mu, delta, and kappa receptors. All the classes, while exhibiting differing modes of action, share some basic similarities. They all are driven by the potassium pump mechanism, which is found on the plasma membrane of the majority of cells.

www.MedChemExpress.com 135 Opioid Receptor Inhibitors & Modulators

ADL-5859 Cat. No.: HY-13044 (Metorphamide) Cat. No.: HY-P1087

Bioactivity: ADL5859 is a δ-opioid receptor agonist with Ki of 0.8 nM, Bioactivity: Adrenorphin is a opioid octapeptide, acting as a potent

selectivity against opioid receptor κ, μ, and weak inhibitory agonist of μ-opioid receptor, with Ki of 12 nM. activity at the hERG channel.

Purity: 99.65% Purity: 95.49% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg 5 mg, 10 mg, 50 mg, 100 mg

Alvimopan dihydrate (ADL 8-2698; LY 246736) Cat. No.: HY-13243 (ADL 8-2698 dihydrate; LY 246736 dihydrate) Cat. No.: HY-76657A

Bioactivity: Alvimopan(LY 246736; ADL 8-2698) is a peripherally acting Bioactivity: Alvimopan dihydrate (ADL 8-2698 dihydrate; LY 246736 mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for dihydrate) is a peripherally acting mu-opioid receptor accelerating gastrointestinal recovery after surgery. IC50 (PAM-OR, IC50= 1.7 nM) antagonist for accelerating Value: 1.7 nM (Mu-type opioid receptor) [1] Target: mu-opioid gastrointestinal recovery after surgery. IC50 Value: 1.7 nM receptor in vitro: The dissociation rate of alvimopan from the… (Mu-type opioid receptor) [1] Target: mu-opioid receptor in… Purity: >98% Purity: 98.02% Clinical Data: Launched Clinical Data: Launched Size: 5 mg, 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

Alvimopan monohydrate AR-M 1000390 hydrochloride (ADL 8-2698 monohydrate; LY 246736 monohydrate) Cat. No.: HY-76657 Cat. No.: HY-101039A

Bioactivity: Alvimopan monohydrate (ADL 8-2698 monohydrate; LY 246736 Bioactivity: AR-M 1000390 hydrochloride is an exceptionally selective,

monohydrate) is a peripherally acting mu-opioid receptor potent δ opioid receptor agonist with an EC50 of 7.2±0.9 (PAM-OR, IC50= 1.7 nM) antagonist for accelerating nM for δ agonist potency. gastrointestinal recovery after surgery.

Purity: 99.18% Purity: 99.80% Clinical Data: Launched Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Asimadoline Aticaprant (EMD-61753) Cat. No.: HY-107384 (CERC-501; LY-2456302) Cat. No.: HY-101718

Bioactivity: is a potent κ opioid receptor agonist with IC50s Bioactivity: Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a K of 0.807 nM. of 5.6 and 1.2 nM for guinea pig and human recombinant κ i opioid receptor, respectively.

Purity: 99.36% Purity: 99.24% Clinical Data: Phase 3 Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg 1 mg, 5 mg, 10 mg, 20 mg

BAM-22P BAN ORL 24 (Bovine adrenal medulla-22P) Cat. No.: HY-P1331 Cat. No.: HY-13222

Bioactivity: BAM-22P, a highly potent , is a potent opioid Bioactivity: BAN ORL 24 is a potent and selective NOP receptor antagonist. agonist. (IC50 values are 0.27, 2500, 6700 and > 10000 nM for NOP, κ-, μ- and δ-receptors respectively).

Purity: >98% Purity: 95.07% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500u g, 1 mg, 5 mg Size: 10mM x 1mL in Water, 10 mg, 50 mg, 100 mg

136 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Bevenopran (CB-5945; ADL-5945) Cat. No.: HY-100122 (GRT6005) Cat. No.: HY-15536

Bioactivity: Bevenopran is a peripheral μ-opioid receptor antagonist. Bioactivity: Cebranopadol is an analgesic NOP and opioid receptor agonist

with Kis/ EC50s of 0.9 nM/13 nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, 18 nM/110 nM for human NOP, MOP, KOP and delta-opioid peptide (DOP) receptor, respectively.

Purity: >98% Purity: 98.76% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 1 mg, 5 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

Cebranopadol ((1α,4α)stereoisomer) CYT-1010 (GRT6005 (1α,4α)stereoisomer) Cat. No.: HY-15536A Cat. No.: HY-123534

Bioactivity: Cebranopadol ((1α,4α)stereoisomer) is a stereoisomer of Bioactivity: CYT-1010 is a mu-opioid receptor agonist extracted from cebranopadol. Cebranopadol is a potent agonist activity on patent WO2013173730A2, with EC50s of 13.1 nM and 0.0053 nM ORL-1. on beta-arrestin recruitment and inhibition of cAMP production, respectively [1]. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg 5 mg, 10 mg, 50 mg

CYT-1010 hydrochloride DAMGO Cat. No.: HY-123534A Cat. No.: HY-P0210

Bioactivity: CYT-1010 hydrochloride is a mu-opioid receptor agonist Bioactivity: DAMGO is a μ-opioid receptor ( μ-OPR ) selective agonist.

extracted from patent WO2013173730A2, with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively [1]. Purity: >98% Purity: 98.10% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 100 mg, 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg

Deltorphin 2 I ([D-Ala2]-Deltorphin II) Cat. No.: HY-P1013 (Deltorphin 1; Deltorphin C) Cat. No.: HY-P1336

Bioactivity: Deltorphin 2 is a selective peptide agonist for the δ opioid Bioactivity: is a δ-opioid receptor agonist with high affinity receptor. and selectivity.

Purity: 98.20% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 25 mg Size: 1 mg, 5 mg, 10 mg

Dermorphin Dynorphin A (1-10) TFA Cat. No.: HY-P0244 Cat. No.: HY-P1594A

Bioactivity: is a natural heptapeptide μ-opioid receptor ( Bioactivity: Dynorphin A (1-10) (TFA), an endogenous opioid neuropeptide, MOR) agonist found in amphibian skin. binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) (TFA) also blocks NMDA-activated current

with an IC50 of 42.0 μM.

Purity: 99.64% Purity: 95.04% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 25 mg Size: 1 mg, 5 mg, 10 mg

www.MedChemExpress.com 137

Dynorphin A 1-10 1-13 Cat. No.: HY-P1594 Cat. No.: HY-P1337

Bioactivity: Dynorphin A (1-10) an endogenous opioid neuropeptide, binds to Bioactivity: Dynorphin B (1-13) acts as an agonist on opioid κ-receptor. extracellular loop 2 of the κ-opioid receptor. Dynorphin A

(1-10) also blocks NMDA-activated current with an IC50 of 42.0 μM.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg

Endomorphin 1 2 Cat. No.: HY-P0185 Cat. No.: HY-P0186

Bioactivity: Endomorphin 1, a high affinity, highly selective agonist of Bioactivity: Endomorphin 2, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for the μ-opioid receptor, displays reasonable affinities for

kappa 3 binding sites, with Ki value between 20 and 30 nM. kappa 3 binding sites, with Ki value between 20 and 30 nM.

Purity: 98.15% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 5 mg, 10 mg, 25 mg 5 mg, 10 mg, 25 mg

Endomorphin 2 TFA Gluten B5 Cat. No.: HY-P0186A Cat. No.: HY-P1742

Bioactivity: Endomorphin 2 TFA, a high affinity, highly selective agonist Bioactivity: Gluten Exorphin B5 is an exogenous opioid peptides derived of the μ-opioid receptor, displays reasonable affinities for from wheat gluten, acts on opioid receptor, increases [1] kappa 3 binding sites, with Ki value between 20 and 30 nM postprandial plasma insulin level in rats . [1]. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 5 mg, 10 mg, 25 mg

Gluten Exorphin C -7 Cat. No.: HY-P1596 Cat. No.: HY-P0318

Bioactivity: Gluten exorphin C is an opioid peptide derived from wheat Bioactivity: Hemorphin-7 is a hemorphin peptide, an endogenous opioid

gluten. Its IC50 values are 40 μM and 13.5 μM for μ opioid and peptide derived from the β-chain of hemoglobin. Hemorphin δ opioid activities in the GPI and MVD assays, respectively. peptides exhibits antinociceptive and antihypertensive activities, activating opioid receptors and inhibiting angiotensin-converting enzyme (ACE). Purity: >98% Purity: 99.65% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 25 mg Size: 1 mg, 5 mg, 10 mg

JDTic JDTic dihydrochloride Cat. No.: HY-10486 Cat. No.: HY-10487

Bioactivity: JDTic is a highly selective antagonist for the κ-opioid Bioactivity: JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptor; without affecting the μ- or δ-opioid receptors. receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.

Purity: >98% Purity: 99.79% Clinical Data: Phase 1 Clinical Data: Phase 1 Size: 5 mg, 10 mg, 50 mg Size: 10mM x 1mL in Water, 5 mg, 10 mg, 50 mg

138 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

JTC-801 Cat. No.: HY-13274 Cat. No.: HY-10827

Bioactivity: JTC-801 is a selective opioid receptor-like1 (ORL1) receptor Bioactivity: Kelatorphan is a full inhibitor of degrading

antagonist, binding to ORL1 receptor with a Ki value of enzymes. 8.2nM.

Purity: 99.73% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg Size: 500 mg, 250 mg

Loperamide hydrochloride LY-2940094 (R-18553 (hydrochloride)) Cat. No.: HY-B0418A Cat. No.: HY-114452

Bioactivity: (hydrochloride) (R-18553 (hydrochloride)) is an Bioactivity: LY-2940094 is a potent, selective and orally available opioid receptor agonist for the treatment of diarrhea. ( NOP receptor) antagonist with high

affinity ( Ki=0.105 nM) and antagonist potency ( Kb=0.166 nM). LY-2940094 reduces self-administration in ani…

Purity: 99.69% Purity: 99.56% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

LY2795050 Cat. No.: HY-15708 (Matridin-15-one; Vegard; α-Matrine) Cat. No.: HY-N0164

Bioactivity: LY2795050 is a novel selective κ-opioid Receptor (KOR) Bioactivity: Matrine (Matridin-15-one) is an alkaloid found in plants from antagonist (IC50=0.72 nM) and has the potential as a PET the Sophora genus. It has a variety of pharmacological tracer to image KOR in vivo. IC50 Value: 0.72 nM (κ-opioid effects, including anti-cancer effects, and action as a kappa Receptor); 25.8 nM (κ-opioid) [1] Target: κ-opioid Receptor in opioid receptor and u-receptor agonist. vitro: LY2795050 displays full antagonist activity and high… Purity: 98.02% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 100 mg, 200 mg, 500 mg

MCOPPB triHydrochloride MT-7716 free base (MCOPPB 3HCl) Cat. No.: HY-13101 (W-212393) Cat. No.: HY-107094A

Bioactivity: MCOPPB 3Hcl is a nociceptin receptor agonist with pKi of Bioactivity: MT-7716 free base (W-212393) is a selective non-peptide 10.07; weaker activity at other opioid receptors. IC50 value: nociceptin receptor (NOP) agonist and promising potential 10.07 (pKi) Target: nociceptin receptor MCOPPB treatment drug for alcohol abuse and relapse prevention [1]. trihydrochloride is a trihydrochloride form of MCOPPB that is a new nonpeptide nociceptin/orphanin FQ peptide (NOP)-receptor… Purity: 99.35% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

MT-7716 hydrochloride N- (W-212393 hydrochloride) Cat. No.: HY-107094 (Norclozapine; Desmethylclozapine; Normethylclozapine) Cat. No.: HY-G0021

Bioactivity: MT-7716 hydrochloride (W-212393 hydrochloride) is a selective Bioactivity: N-Desmethylclozapine is a dengue virus inhibitor, and an non-peptide nociceptin receptor (NOP) agonist and promising agonist of δ-opioid receptor. potential treatment drug for alcohol abuse and relapse prevention [1].

Purity: >98% Purity: 98.66% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 100 mg, 500 mg, 250 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg

www.MedChemExpress.com 139

Naloxegol oxalate (NKTR-118; AZ-13337019) Cat. No.: HY-A0118 (NKTR-118 oxalate; AZ-13337019 oxalate) Cat. No.: HY-A0118A

Bioactivity: Naloxegol (NKTR-118; AZ-13337019) is an opioid-receptor Bioactivity: Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is antagonist [1]. an opioid-receptor antagonist [1].

Purity: >98% Purity: 99.90% Clinical Data: Launched Clinical Data: Launched Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Naltrindole hydrochloride Neuropeptide AF (93-110), Human Cat. No.: HY-101177 (Neuropeptide AF (human)) Cat. No.: HY-P1246

Bioactivity: hydrochloride is a highly potent and selective Bioactivity: Neuropeptide AF (93-110), Human is an endogenous antiopioid

non-peptide δ opioid receptor antagonist with a Ki of 0.02 nM. peptide.

Purity: 99.68% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 500u g, 1 mg, 5 mg 5 mg, 10 mg, 25 mg, 50 mg

Nociceptin Nociceptin (1-13), amide (Orphanin FQ) Cat. No.: HY-P0183 Cat. No.: HY-P1317

Bioactivity: Nociceptin, a heptadecapeptide, is the endogenous ligand of Bioactivity: Nociceptin (1-13), amide is a potent ORL1 (OP4) receptor the nociceptin receptor, acting as a potent anti-analgesic. agonist with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain membranes [1] [2].

Purity: 99.79% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 1 mg, 5 mg, 10 mg, 25 mg

Opioid receptor modulator 1 ORL1 antagonist 1 Cat. No.: HY-U00420 Cat. No.: HY-112263

Bioactivity: Opioid receptor modulator 1 is a opioid receptor modulator Bioactivity: ORL1 antagonist 1 is an opioid receptor-like 1 ( ORL1)

extracted from patent WO2014072809A2, Compound RA11 in antagonist with an IC50 of 61 nM. EXAMPLE 7.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 25 mg Size: 250 mg, 500 mg

PZM21 hydrochloride Cat. No.: HY-101386 (Cucoline hydrochloride) Cat. No.: HY-15122A

Bioactivity: PZM21 is a potent and selective μ opioid receptor agonist Bioactivity: Sinomenine hydrochloride is a blocker of the NF-κB activation

with an EC50 of 1.8 nM. and also an activator of μ-opioid receptor.

Purity: 99.45% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg 100 mg

140 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

SR17018 Cat. No.: HY-111454 Cat. No.: HY-B0380

Bioactivity: SR17018 is an mu-opioid-receptor (MOR) agonist, binding Bioactivity: Trimebutine is a drug with antimuscarinic and weak mu opioid agonist effects. with GTPγS, with an EC50 of 97 nM.

Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 5 g 5 mg, 10 mg, 50 mg, 100 mg

Trimebutine maleate Tyr-Gly-Gly-Phe-Met-OH Cat. No.: HY-B0380A (Met-Enkephalin; Methionine enkephalin) Cat. No.: HY-P0073

Bioactivity: Trimebutine maleate is a drug with antimuscarinic and weak mu Bioactivity: Tyr-Gly-Gly-Phe-Met-OH regulates human immune function and opioid agonist effects. inhibits tumor growth via binding to the opioid receptor.

Purity: 99.95% Purity: 99.81% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 g 10 mg, 25 mg, 50 mg, 100 mg

Valorphin Vanilpyruvic acid Cat. No.: HY-P1599 (Vanylpyruvic acid) Cat. No.: HY-101416

Bioactivity: is an endogenous hemoglobin β-chain (33-39) fragment Bioactivity: Vanilpyruvic acid is a catecholamine metabolite and precursor with opioid analgesic activity, binds to rat mu-opioid to vanillactic acid.

receptor, with an IC50 of 14 nM; Valorphin also shows anti-tumor activity.

Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 25 mg Size: 10mM x 1mL in DMSO, 10 mg

ZT 52656A hydrochloride [D-Ala2]leucine-enkephalin Cat. No.: HY-101582 Cat. No.: HY-P0098

Bioactivity: ZT 52656A is a selective kappa opioid agonist, used for the Bioactivity: [D-Ala2]leucine-enkephalin, a delta opioid agonist, is a prevention or alleviation of pain in the eye. degradation resistant long-acting Leu-enkephalin.

Purity: >98% Purity: 99.75% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in Water, 5 mg, 10 mg, 50 mg

[Leu5]-Enkephalin [Leu5]-Enkephalin, amide (Leu-enkephalin; Leucine enkephalin; Leucyl-enkephalin) Cat. No.: HY-P0288 (Leu-Enkephalin amide) Cat. No.: HY-P1470

Bioactivity: [Leu5]-Enkephalin is a pentapeptides with like Bioactivity: [Leu5]-Enkephalin, amide is a δ opioid receptor agonist. properties. [Leu5]-Enkephalin is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.

Purity: 99.72% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10 mg, 25 mg 10 mg, 25 mg

www.MedChemExpress.com 141

[Met5]-Enkephalin, amide β-, bovine (5-Methionine-enkephalin amide) Cat. No.: HY-P1467 (β-Casomorphin-7 (bovine); Bovine β-casomorphin-7) Cat. No.: HY-P0179

Bioactivity: [Met5]-Enkephalin, amide is an agonist for δ opioid Bioactivity: β-casomorphin, bovine (β-casomorphin-7) is a opioid peptide

receptors as well as putative ζ ζ opioid receptors. with an IC50 of 14 μM in an Opioid receptors binding assay.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mg, 25 mg Size: 5 mg, 10 mg, 25 mg

β-Casomorphin, human β-Endorphin, human (Human β-casomorphin 7) Cat. No.: HY-P1481 Cat. No.: HY-P1502

Bioactivity: β-Casomorphin, human is an opioid peptide, acts as an agonist Bioactivity: β-Endorphin, human, a prominent endogenous peptide, existing of opioid receptor. in the hypophysis cerebri and hypothalamus, is an agonist of opioid receptor, with preferred affinity for μ-opioid receptor and δ-opioid receptor; β-Endorphin, human exhibits antinociception activity. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 25 mg Size: 1 mg, 5 mg, 10 mg

142 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Serotonin Transporter 5-HTT;SERT;SLC6A4

Serotonin Transporters (SERTs) are integral membrane proteins that transport serotonin from synaptic spaces into presynaptic neurons. SERTs function by reuptaking serotonin in the synaptic cleft, effectively terminating the function of serotonin and halting neuronal transmission. Serotonin reuptake is a critical process to prevent overstimulation of nerves. Serotonin transporter (SERT) regulates extracellular levels of serotonin (5-hydroxytryptamine, 5HT) in the brain by transporting 5HT into neurons and glial cells. The human SERT (hSERT) is the primary target for drugs used in the treatment of emotional disorders, including depression. hSERT belongs to the solute carrier 6 family that includes a bacterial leucine transporter (LeuT), for which a high resolution crystal structure has become available.

www.MedChemExpress.com 143 Serotonin Transporter Inhibitors & Modulators

Amitifadine hydrochloride Azaphen (Azafen; Pipofezin hydrochloride; (DOV-21947 hydrochloride; EB-1010 hydrochloride) Cat. No.: HY-18332A hydrochloride) Cat. No.: HY-A0022

Bioactivity: Amitifadine hydrochloride is a Bioactivity: Pipofezine(Azafen or Azaphen) is a potent inhibitor of the serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI), reuptake of serotonin.

with IC50s of 12, 23, 96 nM for serotonin, norepinephrine and dopamine in HEK 293 cells , respectively.

Purity: 99.92% Purity: >98% Clinical Data: Phase 3 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg, 500 mg 5 mg, 10 mg, 50 mg

Azaphen dihydrochloride monohydrate (Azafen dihydrochloride Centanafadine monohydrate; Pipofezin dihydrochloride monohydrate; …) Cat. No.: HY-A0022A (EB-1020) Cat. No.: HY-16736

Bioactivity: Pipofezine(Azafen or Azaphen) is a potent inhibitor of the Bioactivity: Centanafadine is dual norepinephrine (NE)/dopamine (DA) reuptake of serotonin. transporter inhibitor, also inhibits serotonin transporter,

with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.

Purity: 99.60% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 100 mg, 500 mg Size: 250 mg, 500 mg

Centanafadine hydrochloride Cinchonidine (EB-1020 (hydrochloride)) Cat. No.: HY-16736A (α-) Cat. No.: HY-N0173

Bioactivity: Centanafadine (hydrochloride) is dual norepinephrine Bioactivity: Cinchonidine (α-Quinidine) is a cinchona alkaloid found in (NE)/dopamine (DA) transporter inhibitor, also inhibits Cinchona officinalis and Gongronema latifolium. A building block used in asymmetric synthesis in organic chemistry. Weak serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for inhibitor of serotonin transporter (SERT) with K s of 330, human NE, DA and serotonin transporter , respectively. i 4.2, 36, 196, 15 μM for dSERT, hSERT, hSERT I172M, hSERT… Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 100 mg

Citalopram hydrobromide Clomipramine D3 ((±)- hydrobromide; Lu 10-171) Cat. No.: HY-B1287 Cat. No.: HY-B0457AS

Bioactivity: Citalopram hydrobromide is an antidepressant drug of the Bioactivity: Clomipramine D3 is the deuterium labeled Clomipramine, which selective serotonin reuptake inhibitor (SSRI) class. It has US is a highly selective inhibitor of serotonin reuptake. FDA approval to treat major depression.

Purity: 99.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 10 mg, 50 mg, 100 mg

Clomipramine hydrochloride hydrochloride Cat. No.: HY-B0457 (LY-210448 hydrochloride) Cat. No.: HY-B0304A

Bioactivity: Clomipramine HCl is a serotonin transporter (SERT), Bioactivity: Dapoxetine HCl is a short-acting novel selective serotonin norepinephrine transporter (NET) dopamine transporter (DAT) reuptake inhibitor(SSRI). blocker with Ki of 0.14, 54 and 3 nM, respectively. Target: 5-HT Receptor Clomipramine hydrochloride (Anafranil) is a hydrochloride salt of clomipramine which is a serotonin… Purity: 99.72% Purity: 99.85% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 50 mg, 100 mg

144 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Dasotraline Dasotraline hydrochloride (SEP 225289) Cat. No.: HY-12850 (SEP-225289 hydrochloride) Cat. No.: HY-12850A

Bioactivity: Dasotraline is a triple reuptake inhibitor that blocks Bioactivity: Dasotraline hydrochloride (SEP-225289 hydrochloride) is a dopamine, norepinephrine, and serotonin transporters with triple reuptake inhibitor that blocks dopamine,

IC50 values of 4, 6, and 11 nM, respectively. norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.

Purity: >98% Purity: 99.60% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 1 mg, 5 mg, 10 mg, 25 mg, 50 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

Desvenlafaxine succinate hydrate (O-Desmethylvenlafaxine) Cat. No.: HY-B0602 (O-Desmethylvenlafaxine succinate hydrate) Cat. No.: HY-B0602A

Bioactivity: Desvenlafaxine is a serotonin (5-HT) and norepinephrine (NE) Bioactivity: Desvenlafaxine succinate hydrate is an antidepressant of the reuptake inhibitor with Ki of 40.2 nM and 558.4 nM, serotonin-norepinephrine reuptake inhibitor (SNRI). respectively.

Purity: 98.0% Purity: 99.76% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 10 mg, 50 mg

Dopamine serotonin antagonist-1 DOV-216,303 Free Base Cat. No.: HY-42110 Cat. No.: HY-18332C

Bioactivity: Dopamine serotonin antagonist-1 is a dual dopamine and Bioactivity: DOV-216,303 (Free Base) is a potent triple serotonin,

serotonin receptor antagonist with Kis of 200, 2500, 420, 39, norepinephrine, and dopamine reuptake inhibitor, with IC50 84, 40 nM for dopamine D1, D2,D4, and serotonin S2A, S2C, S3, values of 14 nM, 20 nM and 78 nM for hSERT, hNET and hDAT, respectively. respectively [1]. Has antidepressant-like effects … Purity: 99.79% Purity: 98.47% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 5 mg

Doxepin Hydrochloride DSP-1053 Cat. No.: HY-B0725 Cat. No.: HY-111419

Bioactivity: HCl is a that is marketed Bioactivity: DSP-1053 is a potent Serotonin Transporter (SERT) ( Ki=1.02 worldwide. nM) inhibitor with partial 5-HT1A receptor ( Ki=5.05 nM) agonistic activity.

Purity: 99.41% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 500 mg, 100 mg, 250 mg 1 g, 5 g, 10 g

Duloxetine hydrochloride ((S)-Duloxetine; LY248686) Cat. No.: HY-B0161 ((S)-Duloxetine hydrochloride; LY-248686 hydrochloride) Cat. No.: HY-B0161A

Bioactivity: Duloxetine is a serotonin-norepinephrine reuptake inhibitor Bioactivity: Duloxetine hydrochloride is a serotonin-norepinephrine with Ki of 4.6 nM, used for treatment of major depressive reuptake inhibitor (SNRI) with Ki of 4.6 nM, used for disorder and generalized anxiety disorder (GAD). treatment of major depressive disorder and generalized anxiety disorder (GAD).

Purity: >98% Purity: 99.92% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 145

Eplivanserin mixture (SR-46349 (mixture)) Cat. No.: HY-10792A ((S)-Citalopram; S-(+)-Citalopram) Cat. No.: HY-14258

Bioactivity: Eplivanserin mixture is a selective serotonin reuptake Bioactivity: Escitalopram is a selective serotonin reuptake inhibitor (SSRI) with Ki of 0.89 nM. Target: SSRIs Escitalopram, the inhibitor and a 5-HT2A receptor antagonist, extracted from S-enantiomer of citalopram, belongs to a class of patent WO 2005/002578 A1 [1]. antidepressant agents known as selective serotonin-reuptake inhibitors (SSRIs). Escitalopram may be used to treat major… Purity: 99.95% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Escitalopram oxalate ((S)-(+)Citalopram oxalate) Cat. No.: HY-14258A (LY-110140 (free base)) Cat. No.: HY-B0102

Bioactivity: Escitalopram is a selective serotonin reuptake inhibitor Bioactivity: Fluoxetine (LY-110140 free base) is a selective serotonin (SSRI) with Ki of 0.89 nM. reuptake inhibitor ( SSRI) class used for antidepressant research.

Purity: 98.0% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 50 mg, 100 mg, 500 mg 10 mg, 50 mg, 100 mg

Fluoxetine hydrochloride (LY-110140) Cat. No.: HY-B0102A (DU-23000) Cat. No.: HY-B0103

Bioactivity: Fluoxetine hydrochloride is an antidepressant and a selective Bioactivity: Fluvoxamine (DU-23000) is an antidepressant which functions serotonin reuptake inhibitor. pharmacologically as a selective serotonin reuptake inhibitor.

Purity: 99.86% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg, 100 mg 50 mg, 100 mg, 500 mg

Fluvoxamine maleate hydrochloride (DU-23000 (maleate)) Cat. No.: HY-B0103A Cat. No.: HY-B1490

Bioactivity: Fluvoxamine (maleate) (DU-23000 (maleate)) is an Bioactivity: Imipramine hydrochloride inhibits serotonin transporter with an antidepressant which functions pharmacologically as a IC50 value of 32 nM in vitro. selective serotonin reuptake inhibitor.

Purity: 99.85% Purity: 99.89% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 10 mg, 50 mg, 100 mg 100 mg

Milnacipran (1S-cis) hydrochloride Cat. No.: HY-B0168 ( hydrochloride; F-2695 hydrochloride) Cat. No.: HY-B0168B

Bioactivity: Milnacipran is a serotonin-norepinephrine reuptake inhibitor Bioactivity: Milnacipran (1S-cis) hydrochloride is a (SNRI) used in the clinical treatment of fibromyalgia. serotonin-norepinephrine reuptake inhibitor (SNRI), used in the clinical treatment of fibromyalgia.

Purity: >98% Purity: 99.94% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in Water, 5 mg, 10 mg, 50 mg

146 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Milnacipran hydrochloride Cat. No.: HY-B0168A (CIBA 2330Go) Cat. No.: HY-101684

Bioactivity: Milnacipran hydrochloride is a serotonin-norepinephrine Bioactivity: Nitroxazepine is a tricyclic antidepressant (TCA) for the reuptake inhibitor (SNRI) used in the clinical treatment of treatment of depression. Nitroxazepine acts as a fibromyalgia. serotonin-norepinephrine reuptake inhibitor.

Purity: 99.40% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 10 mg, 50 mg, 100 mg

Paroxetine hydrochloride hydrochloride hemihydrate (BRL29060 hydrochloride (BRL29060 hydrochloride; BRL29060A) Cat. No.: HY-B0492 hemihydrate; BRL29060A hemihydrate) Cat. No.: HY-B0492A

Bioactivity: Paroxetine hydrochloride is a potent selective Bioactivity: Paroxetine hydrochloride hemihydrate is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an serotonin-reuptake inhibitor, commonly prescribed as an

antidepressant and has GRK2 inhibitory ability with IC50 of antidepressant and has GRK2 inhibitory ability with IC50 of 14μM. 14μM.

Purity: 99.0% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg, 500 mg 100 mg, 500 mg

Sertraline hydrochloride SPD-473 citrate Cat. No.: HY-B0176A Cat. No.: HY-101612

Bioactivity: hydrochloride is an antidepressant of the selective Bioactivity: SPD-473 citrate is a serotonin/ dopamine/ norepinephrine serotonin reuptake inhibitor (SSRI) class. reuptake inhibitior.

Purity: 99.90% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 50 mg

Venlafaxine hydrochloride (Wy 45030) Cat. No.: HY-B0196 (Wy 45030 hydrochloride) Cat. No.: HY-B0196A

Bioactivity: Venlafaxine is an antidepressant of the Bioactivity: Venlafaxine hydrochloride is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class. serotonin-norepinephrine reuptake inhibitor (SNRI) class.

Purity: >98% Purity: 99.87% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg Size: 10mM x 1mL in Water, 10 mg, 50 mg

Vilazodone Vilazodone D8 (EMD 68843; SB659746A) Cat. No.: HY-14262 Cat. No.: HY-14261S

Bioactivity: Vilazodone (EMD 68843; SB 659746A) is a combined serotonin Bioactivity: Vilazodone D8 is the a deuterium labeled vilazodone, which is specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial a combined serotonin specific reuptake inhibitor (SSRI) and agonist currently under clinical evaluation for the treatment 5-HT1A receptor partial agonist. of major depression.

Purity: 99.91% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg 10 mg, 50 mg

www.MedChemExpress.com 147

Vilazodone Hydrochloride Vortioxetine (EMD 68843 (Hydrochloride); SB659746A (Hydrochloride)) Cat. No.: HY-14261 (Lu AA 21004) Cat. No.: HY-15414

Bioactivity: Vilazodone Hydrochloride (EMD 68843 Hydrochloride; SB659746A Bioactivity: Vortioxetine is a inhibitor of 5-HT1A, 5-HT1B, 5-HT3A, Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT receptor and SERT, with K values of 15 nM, 33 nM, 5-HT receptor partial agonist. 7 i 1A 3.7 nM, 19 nM and 1.6 nM, respectively.

Purity: 99.94% Purity: 98.81% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 50 mg

Vortioxetine hydrobromide Wf-516 (Lu AA21004 hydrobromide) Cat. No.: HY-15414A Cat. No.: HY-19417A

Bioactivity: Vortioxetine hydrobromide is a multimodal serotonergic agent, Bioactivity: Wf-516 is an inhibitor of 5-HT reuptake, and an antagonist inhibits 5-HT , 5-HT , 5-HT , 5-HT receptor and 1A 1B 3A 7 of 5-HT1A and 5-HT2A receptors, with Ki of 5 nM and 40 nM

SERT with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 for 5-HT1A receptor and 5-HT2A receptor in humans, nM, respectively. respectively, and has potent antidepressant activity. Purity: 99.54% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 50 mg

148 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] γ-secretase Gamma secretase

The γ-secretases are intramembrane cleaving protein complexes responsible for the generation of amyloid β (Aβ) from the amyloid precursor protein (APP). Apart from presenilins (PSEN) , a mature and active γ-secretase complex consists of three additional subunits: Nicastrin (Nct), PSEN enhancer 2 (Pen-2), and either anterior pharynx 1 (APH-1) A or B. The γ-secretase complexes proteolyse type 1 transmembrane proteins, among them the APP, the Notch receptors and ligands, the Erb4 receptor and N-Cadherin. Inhibition of γ-secretase with DAPT significantly reduced the production of extracellular Aβ38, Aβ40, and Aβ42 in neurons of all genotypes. Compounds that inhibit or modulate γ-secretase can be considered as a potential therapeutics for AD because their use appears to be a rational strategy to prevent senile plaque (SP) formations.

www.MedChemExpress.com 149 γ-secretase Inhibitors & Modulators

Avagacestat Begacestat (BMS-708163) Cat. No.: HY-50845 (GSI-953) Cat. No.: HY-14175

Bioactivity: Avagacestat (BMS-708163) is a potent inhibitor of Bioactivity: Begacestat (GSI-953) is a selective thiophene

γ-secretase, with IC50s of 0.27 nM and 0.30 nM for Aβ42 and inhibitor of amyloid precursor protein gamma-secretase (IC Aβ40 inhibition; Avagacestat (BMS-708163) also inhibits NICD 50Aβ 40=15 nM) for the treatment of Alzheimer's disease [1] (Notch IntraCellular Domain) with IC50 of 0.84 nM and sh… . Purity: 99.93% Purity: 99.0% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg 5 mg, 10 mg, 50 mg

BI-1408 BMS 299897 Cat. No.: HY-112282 Cat. No.: HY-50883

Bioactivity: BI-1408 is a potent γ secretase modulator with an IC50 of Bioactivity: BMS 299897 is a sulfonamide γ-secretase inhibitor with an [1] IC50 of 7 nM for Aβ production inhibition in HEK293 cells 0.04 μM for Aβ42 . stably overexpressing amyloid precursor protein (APP).

Purity: >98% Purity: 99.35% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 100 mg, 250 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

BMS 433796 Compound E Cat. No.: HY-50884 (Compound E (secretase inhibitor)DuPont E) Cat. No.: HY-14176

Bioactivity: BMS 433796 is a γ-secretase inhibitor with Aβ lowering Bioactivity: Compound E is a γ-secretase inhibitor. Compound E bloks activity in a transgenic mouse model of Alzheimer's disease. β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage

with IC50s of 0.24, 0.37, 0.32 nM, respectively.

Purity: >98% Purity: 99.87% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg

DAPT E 2012 (GSI-IX) Cat. No.: HY-13027 Cat. No.: HY-10016

Bioactivity: DAPT is a γ-secretase inhibitor with IC50s of 115 and 200 nM Bioactivity: E 2012 is a potent γ-secretase modulator. IC50 value: Target: for total Aβ and Aβ42, respectively. γ-secretase In the present study, 9 dogs were treated with a single dose of the γ-secretase modulator E2012, the γ-secretase inhibitor LY450139, or vehicle with a dosing interval of 1 week. The isoform Aβ(1-37) was significantly… Purity: 99.97% Purity: 96.91% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 100 mg

ELN 318463 racemate gamma-secretase modulator 1 Cat. No.: HY-50882A Cat. No.: HY-10043

Bioactivity: ELN 318463 racemate is the racemate of ELN 318463. ELN 318463 Bioactivity: γ-secretase inhibitior-1 is a gamma-secretase modulator, is a selective gamma-secretase inhibitor. γ-secretase inhibitior-1 is useful for Alzheimer's disease.

Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10 mg, 100 mg

150 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

gamma-secretase modulator 2 gamma-secretase modulator 3 Cat. No.: HY-50754 Cat. No.: HY-50889

Bioactivity: gamma-secretase modulator 2 is a potent and selective Bioactivity: gamma-secretase modulator 3 is a gamma-secretase modulator. γ-secretase modulator for treatment of Alzheimer's disease.

Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10 mg, 100 mg 10 mg, 50 mg

Itanapraced L-685458 (CHF5074; CSP-1103) Cat. No.: HY-14399 (L-685,458) Cat. No.: HY-19369

Bioactivity: Itanapraced (CHF5074) is a novel γ-secretase modulator, Bioactivity: L-685458 is a potent inhibitor of Amyloid β-Protein precursor reduces Aβ42 and Aβ40 secretion, with an IC50 of 3.6 and 18.4 γ-secretase activity with IC50 of 17 nM, shows greater than μM, respectively. 50-100-fold selectivity over other aspartyl proteases tested.

Purity: 98.0% Purity: 99.78% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg

LY-411575 LY-411575 isomer 1 Cat. No.: HY-50752 Cat. No.: HY-50752A

Bioactivity: LY-411575 is a potent γ-secretase inhibitor with IC50 of Bioactivity: LY-411575 isomer 1 is an isomer of LY411575, which is a potent 0.078 nM/0.082 nM (membrane/cell-based), and also inhibits γ-secretase inhibitor.

Notch S3 cleavage with IC50 of 0.39 nM.

Purity: 98.71% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 mg

LY-411575 isomer 2 LY-411575 isomer 3 Cat. No.: HY-50752B Cat. No.: HY-50752C

Bioactivity: LY-411575 isomer 2 is an isomer of LY411575, which is a potent Bioactivity: LY-411575 isomer 3 is an isomer of LY411575, which is a potent γ-secretase inhibitor. γ-secretase inhibitor.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg 1 mg

MK-0752 MRK-560 Cat. No.: HY-10974 Cat. No.: HY-14174

Bioactivity: MK-0752 is a moderately potent γ-secretase inhibitor, which Bioactivity: MRK-560 is a potent, orally bioavailable and brain-penetrant reduces Aβ40 production with IC50 of 5 nM. γ-secretase inhibitor [1].

Purity: 98.87% Purity: 99.0% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 151

NGP555 Nirogacestat Cat. No.: HY-108714 (PF-3084014; PF-03084014) Cat. No.: HY-15185

Bioactivity: NGP555 is a γ-secretase modulator. Bioactivity: Nirogacestat (PF-3084014) is a reversible, noncompetitive, and

selective γ-secretase inhibitor with IC50 of 6.2 nM.

Purity: >98% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

RO4929097 Semagacestat (RG-4733) Cat. No.: HY-11102 (LY450139) Cat. No.: HY-10009

Bioactivity: RO4929097 (RG-4733) is a γ secretase inhibitor with IC50 of Bioactivity: Semagacestat is a γ-secretase inhibitor, inhibits β-amyloid ( Aβ42), Aβ38 and Aβ40 with IC of 10.9, 12 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC 50

50 of 14 nM and 5 nM, respectively. and 12.1 nM, respectively; also inhibits Notch signaling with IC50 of 14.1 nM. Purity: 98.02% Purity: 98.83% Clinical Data: Phase 2 Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Sulindac sulfide YO-01027 (cis- sulfide) Cat. No.: HY-B1786 (; DBZ) Cat. No.: HY-13526

Bioactivity: Sulindac sulfide is a noncompetitive γ-secretase inhibitor, Bioactivity: YO-01027 (Dibenzazepine;DBZ) is a potent γ-secretase

with an IC50 of 20.2 μM for γ 42-secretase activity. inhibitor with IC50 values of 2.92±0.22 and 2.64±0.30 nM for Notch and APPL cleavage, respectively.

Purity: >98% Purity: 99.23% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 25 mg

Z-Ile-Leu-aldehyde γ-Secretase modulator 4 (Z-IL-CHO; GSI-XII; γ-Secretase inhibitor XII) Cat. No.: HY-12465 Cat. No.: HY-128581

Bioactivity: Z-Ile-Leu-aldehyde(Z-IL-CHO; GSI-XII) is a potent Bioactivity: γ-Secretase modulator 4 is a potent γ-secretase modulator, gamma-Secretase inhibitor; Notch signaling inhibitor. reduces the Aβ42 level with IC50s of 0.014 μM and 0.017 μM in human and mouse, respectively [1].

Purity: 98.10% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 100 mg, 500 mg 5 mg, 10 mg

152 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]