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Inhibitors, , Screening Libraries www.MedChemExpress.com

Membrane Transporter/Ion Channel

Most of molecules enter or leave cells mainly via membrane transport proteins, which play important roles in several cellular functions, including cell , ion homeostasis, signal transduction, binding with small molecules in extracellular space, the recognition process in the immune system, energy transduction, osmoregulation, and physiological and developmental processes. There are three major types of transport proteins, ATP-powered pumps, channel proteins and transporters. ATP-powered pumps are ATPases that use the energy of ATP hydrolysis to move ions or small molecules across a membrane against a chemical concentration gradient or electric potential. Channel proteins transport water or specific types of ions down their concentration or electric potential gradients. Many other types of channel proteins are usually closed, and open only in response to specific signals. Because these types of ion channels play a fundamental role in the functioning of nerve cells. Transporters, a third class of membrane transport proteins, move a wide variety of ions and molecules across cell membranes. Membrane transporters either enhance or restrict distribution to the target organs. Depending on their main function, these membrane transporters are divided into two categories: the efflux (export) and the influx (uptake) transporters. Transport proteins such as channels and transporters play important roles in the maintenance of intracellular homeostasis, and mutations in these transport protein genes have been identified in the pathogenesis of a number of hereditary diseases. In the central nervous system ion channels have been linked to many diseases such, but not limited to, ataxias, paralyses, , and deafness indicative of the roles of ion channels in the initiation and coordination of movement, sensory perception, and encoding and processing of information. Furthermore, drug transporters can serve as drug targets or as a mechanism to facilitate drug delivery to cells and tissues.

References: [1] Sadée W, et al. Pharm Res. 1995 Dec;12(12):1823-37. [2] Girardin F. Dialogues Clin Neurosci. 2006;8(3):311-21. [3] Zaydman MA, et al. Chem Rev. 2012 Dec 12;112(12):6319-33.

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Target List in Membrane Transporter/

• ATP Synthase 3 • Proton Pump 101

• BCRP 6 • SGLT 106

• Channel 8 • Channel 109

• CFTR 22 • TRP Channel 119

• 25 • URAT1 127

• CRAC Channel 28

• CRM1 30

• EAAT2 32

• GABA 34

• GlyT 45

• HCN Channel 47

• iGluR 49

• Monoamine Transporter 61

• Monocarboxylate Transporter 64

• Na+/Ca2+ Exchanger 66

• Na+/HCO3- Cotransporter 68

• Na+/K+ ATPase 70

• nAChR 73

• NKCC 79

• P-glycoprotein 81

• P2X Receptor 85

• Channel 88

www.MedChemExpress.com 3 ATP Synthase

ATPases are a class of that catalyze the decompositionof ATP into ADP and a free phosphate ion. This dephosphorylation reaction releases energy, which the (in most cases) harnesses to drive other chemical reactions that would not otherwise occur. Some such enzymes are integral membrane proteins and move solutes across the membrane, typically against their concentration gradient. These are called transmembrane ATPases. Transmembrane ATPases import many of the metabolites necessary for cell metabolism and export toxins, wastes, and solutes that can hinder cellular processes. Such as the sodium-potassium exchanger (or Na + /K + ATPase) and the hydrogen potassium ATPase (H +/K + ATPase or gastric proton pump) that acidifies the contents of the stomach.

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ATP synthase inhibitor 1 BTB06584 Cat. No.: HY-112715 Cat. No.: HY-15877

Bioactivity: ATP synthase inhibitor 1 is a potent inhibitor of c subunit Bioactivity: BTB06584 is an IF1-dependent selective inhibitor of the mitochondrial F1Fo-ATPase. of the F1/FO-ATP synthase complex, inhibits mitochondrial permeability transition pore (mPTP) opening, does not affect ATP levels [1]. Purity: >98% Purity: 98.48% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 100 mg, 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Gboxin Oligomycin A Cat. No.: HY-111651 (MCH 32) Cat. No.: HY-16589

Bioactivity: Gboxin is an oxidative phosphorylation inhibitor that targets Bioactivity: Oligomycin A, created by Streptomyces, acts as a

glioblastoma. Gboxin inhibits the activity of F0F1 ATP mitochondrial F0F1-ATPase inhibitor, with a Ki of 1 μM; synthase [1]. Antitumour activity [1]. Oligomycin A shows anti-fungal activity.

Purity: 99.32% 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 1 mg, 5 mg

www.MedChemExpress.com 5 BCRP Breast cancer resistance protein;ABCG2

BCRP(breast cancer resistant protein) is an ATP-binding cassette (ABC) transporter, which together with two other ABC efflux drug pumps, namely P-glycoprotein (P-, ABCB1) and multidrug resistance-related protein 1 (MRP1, ABCC1) is the most important multidrug resistance protein found in eukaryotic cells including cells in the testis. Breast cancer resistance protein (BCRP/ABCG2) is known to localize at the blood-brain barrier (BBB) and can significantly restrict xenobiotic permeability in the brain. The objective of this study is to investigate the regulation of BCRP functional expression by peroxisome proliferator-activated receptor alpha (PPARα), a -activated transcription factor primarily involved in lipid metabolism, in a cerebral microvascular endothelial cell culture system (hCMEC/D3), representative of human BBB.

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BCRP-IN-1 Elacridar Cat. No.: HY-100390 (GF120918; GW0918; GG918; GW120918) Cat. No.: HY-50879

Bioactivity: BCRP-IN-1 is a breast cancer resistance protein ( BCRP) Bioactivity: Elacridar is a potent P-glycoprotein (Pgp) and BCRP

inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter. inhibitor.

Purity: 98.13% Purity: 98.47% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg, 100 mg, 200 mg, 500 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Fumitremorgin C Ko 143 (12α-Fumitremorgin C) Cat. No.: HY-N2143 Cat. No.: HY-10010

Bioactivity: Fumitremorgin C is a potent and selective ABCG2/BRCP Bioactivity: Ko 143 is a potent and selective ATP-binding cassette inhibitor. sub-family G member 2 ( ABCG2) inhibitor.

Purity: 99.63% 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, 250u g, 1 mg 5 mg, 10 mg, 50 mg, 100 mg

KS176 YHO-13177 Cat. No.: HY-19753 Cat. No.: HY-12757

Bioactivity: KS176 is a potent and selective inhibitor of the breast cancer Bioactivity: YHO-13177 is a potent and specific inhibitor of BCRP; resistance protein (BCRP) multidrug transporter (IC50 values potentiated the cytotoxicity of SN-38 in cancer cells and no are 0.59 and 1.39 μM in Pheo A and Hoechst 33342 assays effect on P-glycoprotein–mediated resistance in respectively). Displays no inhibitory activity against P-gp or MDR1-transduced human leukemia K562 cells. MRP1. Purity: 99.21% 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

YHO-13351 YHO-13351 free base Cat. No.: HY-12758 Cat. No.: HY-12758A

Bioactivity: YHO-13351 is the water-soluble of YHO-13177, which is Bioactivity: YHO-13351 (free base) is the water-soluble prodrug of a potent and specific inhibitor of BCRP. YHO-13177, which is a potent and specific inhibitor of BCRP.

Purity: >98% Purity: 98.10% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Zamicastat (BIA 5-1058) Cat. No.: HY-106004

Bioactivity: Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor that could cross the blood-brain barrier (BBB) and cause central as well as peripheral effects. Zamicastat is also a concentration-dependent dual P-gp and BCRP inhibitor [1] with IC50 values of 73.8 μM and 17.0 μM, respectively .… Purity: 99.95% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 7 Ca2+ channels;Ca channels

Calcium channel is an ion channel which displays selective permeability to calcium ions. It is sometimes synonymous as voltage-dependent calcium channel, although there are also ligand-gated calcium channels. Voltage-gated calcium (CaV) channels catalyse rapid, highly selective influx of Ca 2+ into cells despite a 70-fold higher extracellular concentration of Na +. Some calcium channel blockers have the added benefit of slowing your rate, which can further reduce blood pressure, relieve chest pain () and control an irregular heartbeat.

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(+)- ABT-639 Cat. No.: HY-B1671 Cat. No.: HY-19721

Bioactivity: (+)-Kavain, a main extracted from Piper Bioactivity: ABT-639 is a novel, peripherally acting, selective T-type methysticum, has anticonvulsive properties, attenuating Ca2+ . vascular smooth muscle contraction through interactions with voltage-dependent Na + and Ca 2+ channels [1]. (+)-Kav…

Purity: 99.98% Purity: 99.15% 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 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

ABT-639 hydrochloride chloride Cat. No.: HY-101616 (Ach; ACh chloride) Cat. No.: HY-B0282

Bioactivity: ABT-639 hydrochloride is a novel, peripherally acting, Bioactivity: Acetylcholine (chloride) is a common found selective T-type Ca2+ channel blocker. in the central and peripheral nerve system.

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

ACT-709478 AE0047 Hydrochloride Cat. No.: HY-112723 Cat. No.: HY-U00284

Bioactivity: ACT-709478 is a potent, selective, orally active, and brain Bioactivity: AE0047 Hydrochloride is a calcium blocker, used in the penetrating T-type . ACT-709478 is used research of hypertensive disease. in the research of generalized epilepsies [1].

Purity: 99.68% 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

Amlodipine besylate Cat. No.: HY-B0317 (Amlodipine benzenesulfonate) Cat. No.: HY-B0317B

Bioactivity: Amlodipine is a long-acting calcium channel blocker. Bioactivity: Amlodipine besylate is a long-acting calcium channel blocker.

Purity: 99.57% Purity: 98.21% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 1 g, 5 g

Amlodipine maleate Cat. No.: HY-B0317A Cat. No.: HY-U00044

Bioactivity: Amlodipine maleate is a long-acting calcium channel blocker. Bioactivity: Anipamil is a long-acting calcium channel blocker, used for the treatment of .

Purity: 99.87% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg 1 g, 5 g

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Aranidipine (MPC1304) Cat. No.: HY-U00212 (CS 905) Cat. No.: HY-B0023

Bioactivity: (MPC1304) is a Ca2+ channel antagonist with Bioactivity: Azelnidipine(CS 905; Calblock) is a novel dihydropyridine potent and long-lasting antihypertensive effects. derivative, a L-type calcium channel blocker, and an antihypertensive.

Purity: >98% Purity: 99.35% Clinical Data: Launched Clinical Data: Launched Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

Azelnidipine D7 Bay-K-8644 ((R)-(+)-) (CS-905 D7) Cat. No.: HY-B0023S ((R)-(+)-Bay-K-8644; R-4407; NI-105; (+)-BAY-K-8644) Cat. No.: HY-15125

Bioactivity: Azelnidipine D7 is deuterium labeled Azelnidipine, which is a Bioactivity: Bay-K-8644 (R)-(+)- is a calcium channel inhibitor. L-type calcium channel blocker. 2+ Bay-K-8644 (R)-(+)- inhibits Ba currents ( IBa) ( IC50=975 nM).

Purity: >98% Purity: 98.90% 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

Bay-K-8644 ((S)-(-)-) hydrochloride ((S)-(-)-Bay-K-8644; (-)-BAY-R-5417; (-)-BAY-K-8644) Cat. No.: HY-15124 (KW-3049) Cat. No.: HY-B1448

Bioactivity: Bay-K-8644 (S)-(-)- is an of L-type Ca2+ channel. Bioactivity: Benidipine hydrochloride is a dihydropyridine calcium channel blocker for the treatment of high blood pressure Bay-K-8644 (S)-(-)- activates Ba 2+ currents ( I ) ( Ba (). EC50=32 nM).

Purity: 98.34% Purity: 99.96% 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

Bepridil hydrochloride Ca2+ channel agonist 1 (CERM 1978) Cat. No.: HY-103315 Cat. No.: HY-41076

Bioactivity: hydrochloride (CERM 1978) is a calcium channel Bioactivity: Ca 2+ channel agonist 1 is an agonist of N-type Ca2+ channel blocker, with activity. and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction. Purity: 99.76% Purity: 99.00% 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, 50 mg

Calcium channel inhibitor 1 Calcium channel-modulator-1 Cat. No.: HY-101096 Cat. No.: HY-U00135

Bioactivity: Calcium channel inhibitor 1 (compound 33) is a potent and Bioactivity: Calcium channel-modulator-1 is a calcium ;

selective inhibitor of the T-type calcium channel. blocks aortic contraction with an IC50 of 0.8 μM.

Purity: 99.82% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

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Carboxyamidotriazole Cav 2.2 blocker 1 (L 651582; CAI) Cat. No.: HY-16126 Cat. No.: HY-119373

Bioactivity: (L 651582; CAI) is a blocker of Bioactivity: Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel [1] non-voltage dependent calcium channel . (Cav 2.2) blocker for the treatment of pain, with an IC50 of Carboxyamidotriazole (L 651582; CAI) is a non-cytotoxic 1 nM [1]. anti-tumor drug, which also shows anti-inflammatory activ…

Purity: 99.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg Size: 100 mg, 500 mg, 250 mg

CDN1163 Cat. No.: HY-101455 (FRC-8653) Cat. No.: HY-17404

Bioactivity: CDN1163 is a sarco/endoplasmic reticulum Ca2+-ATPase ( Bioactivity: Cilnidipine(FRC8653) is a dual L- and N-type calcium channel SERCA) activator. blocker and displays antihypertensive, sympatholytic and neuroprotective activity.

Purity: 99.12% Purity: 99.92% 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 10 mg, 50 mg, 100 mg

Cinnarizine Cat. No.: HY-B1090 Cat. No.: HY-17436

Bioactivity: is an antihistamine and a calcium channel blocker, Bioactivity: Clevidipine is a short-acting dihydropyridine calcium channel promote cerebral blood flow, used to treat cerebral apoplexy, antagonist (IC50= 7.1 nM, V(H) = -40 mV ) under development post-trauma cerebral symptoms, and cerebral arteriosclerosis. for treatment of perioperative hypertension. IC50 Value: 7.1 nM at V(H) = -40 mV [1] Target: calcium channel in vitro: Both clevidipine and completely reversed… Purity: 98.0% Purity: 99.74% 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

CP-060 Cromolyn sodium Cat. No.: HY-U00354 (Disodium Cromoglycate; FPL-670) Cat. No.: HY-B0320A

Bioactivity: CP-​060 is a potent Ca2+ antagonist, inhibits Ca 2+ Bioactivity: Cromolyn sodium is an antiallergic drug. Cromolyn sodium is a overload and possesses antioxidant and cardioprotective GSK-3β inhibitor with an IC50 of 2.0 µM. activities.

Purity: >98% Purity: 99.97% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in Water, 1 g, 5 g

CV-159 Dantrolene sodium Cat. No.: HY-19025 (F 440) Cat. No.: HY-14657

Bioactivity: CV-159 is a unique dihydropyridine Ca2+ antagonist with an Bioactivity: Dantrolene sodium is a inhibitor of calcium channel proteins, anti- (CaM) action, and has antiinflammatory inhibiting the release of Ca2+ from the sarcoplasm. Dantrolene activities. sodium is a skeletal which acts by blocking muscle contraction beyond the neuromuscular junction.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 100 mg, 500 mg

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Dantrolene sodium hemiheptahydrate (Dantrolene sodium hydrate) Cat. No.: HY-12542A (PY 108-068; PY-108068) Cat. No.: HY-U00086

Bioactivity: Dantrolene sodium hemiheptahydrate is a skeletal muscle Bioactivity: Darodipine (PY 108-068, PY-108068) is a potent calcium relaxant which acts by blocking muscle contraction beyond the channel antagonist. neuromuscular junction. Dantrolene sodium hemiheptahydrate is a inhibitor of calcium channel proteins, inhibiting the release of Ca2+ from the sarcoplasm. Purity: 98.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg 100 mg, 200 mg, 500 mg

Dehydronitrosonisoldipine DHBP dibromide Cat. No.: HY-Z0816 (Diheptylviologen dibromide) Cat. No.: HY-101237

Bioactivity: Dehydronitrosonisoldipine is a calcium channel antagonist. Bioactivity: DHBP dibromide is an inhibitor for calcium release and a muscle relaxant.

Purity: 98.79% Purity: 99.56% 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 100 mg

Diltiazem hydrochloride Dopropidil (CRD-401) Cat. No.: HY-14656 Cat. No.: HY-U00151

Bioactivity: hydrochloride is a Ca2+ influx inhibitor (slow Bioactivity: Dopropidil is a novel anti-anginal calcium ion modulating channel blocker or calcium antagonist). agent, possessing intracellular calcium antagonist activity and anti-ischemic effects in several predictive animal models.

Purity: 98.39% 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 1 g, 5 g

Efonidipine hydrochloride (NZ-105; (±)-Efonidipine) Cat. No.: HY-12502 (NZ-105 hydrochloride) Cat. No.: HY-12502B

Bioactivity: Efonidipine(NZ-105) is a dual T-type and L-type calcium Bioactivity: Efonidipine Hcl (NZ-105) is a dual T-type and L-type calcium channel blocker (CCB). IC50 value: Target: calcium channel channel blocker (CCB). blocker in vitro: Efonidipine and , but not other examined CCBs, also increased the N(6), 2'-O-dibutyryladenosine 3',5'-cyclic monophosphate… Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg Size: 10 mg, 50 mg

Efonidipine hydrochloride monoethanolate (NZ-105 hydrochloride monoethanolate) Cat. No.: HY-12502A Cat. No.: HY-B1378

Bioactivity: Efonidipine hydrochloride monoethanolate (NZ-105 hydrochloride Bioactivity: Ethosuximide, a widely prescribed anti-epileptic drug, monoethanolate) is a dual T-type and L-type calcium channel improves the phenotypes of multiple neurodegenerative disease blocker (CCB). IC50 value: Target: calcium channel blocker in models and blocks the low voltage activated T-type calcium vitro: Efonidipine and nifedipine, but not other examined channel. CCBs, also increased the N(6), 2'-O-dibutyryladenosine… Purity: 99.83% Purity: 99.54% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 500 mg

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Etiracetam Etripamil (UCB 6474) Cat. No.: HY-B0106A (MSP-2017; (-)-MSP-2017) Cat. No.: HY-17611

Bioactivity: (UCB 6474) is an acetylcholine agonist and a Bioactivity: Etripamil (MSP-2017) is a short-acting L-type drug of the family. Less active than its calcium-channel antagonist with a rapid onset of action S-enantiomer (UCB L059) [1]. designed for intranasal administration, used to treat Paroxysmal Supraventricular (PSVT). Etripamil (MSP-2017) slows atrioventricular nodal conduction and… Purity: 99.91% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 50 mg

Fantofarone (SR 33557) Cat. No.: HY-105117 (HA-1077; AT877) Cat. No.: HY-10341A

Bioactivity: is a highly potent Calcium Channel antagonist. Bioactivity: Fasudil (HA-1077; AT877), a potent inhibitor of ROCK with a 2+ Ki of 0.33 μM for ROCK1, which is also a potent Ca channel antagonist and vasodilator.

Purity: 98.56% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg, 200 mg, 500 mg 5 mg, 10 mg, 50 mg, 100 mg

Fasudil Hydrochloride (HA-1077 (Hydrochloride); AT-877 (Hydrochloride)) Cat. No.: HY-10341 Cat. No.: HY-B0309

Bioactivity: Fasudil Hydrochloride (HA-1077 Hydrochloride; AT-877 Bioactivity: Felodipine is a long-acting 1,4-dihydropyridine calcium

Hydrochloride), a potent inhibitor of ROCK with a Ki of 0.33 channel blocker. Target: Calcium Channel Felodipine is a long-acting 1,4-dihydropyridine calcium channel blocker μM for ROCK1, which is also a potent Ca2+ channel antagonist (CCB)b. It acts primarily on vascular smooth muscle cells by and vasodilator. stabilizing voltage-gated L-type calcium channels in their… Purity: 99.91% Purity: 99.75% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 200 mg, 500 mg 10 mg, 50 mg

Fendiline hydrochloride Cat. No.: HY-B0984 Cat. No.: HY-B1221

Bioactivity: is a nonselective calcium channel blocker. Bioactivity: Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase ( COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selective cation channel…

Purity: 99.98% Purity: 99.92% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 100 mg

Flunarizine dihydrochloride Fluspirilene Cat. No.: HY-B0358A (R 6218; Redeptin) Cat. No.: HY-B1655

Bioactivity: is a selective calcium entry blocker. Bioactivity: Fluspirilene is a non-competitive antagonist of L-type

calcium channels with an IC50 of 0.03 μM. Fluspirileneis a long-acting injectable depot drug used for .

Purity: 99.76% Purity: 99.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg 500 mg

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Gabapentin enacarbil Cat. No.: HY-A0057 (XP-13512) Cat. No.: HY-16216

Bioactivity: Gabapentin (Neurontin) is a pharmaceutical drug, specifically Bioactivity: (XP-13512) is a prodrug for the a GABA analog. It was originally developed to treat , and drug gabapentin. and currently is also used to relieve . IC50 Value: 140 nM (α2δ subunit of calcium channel) [1] Target: Calcium Channel in vitro: Gabapentin, and CGP 44532… Purity: 98.0% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 5 mg, 10 mg 10 mg, 50 mg, 100 mg

Gabapentin hydrochloride Ginsenoside Rd Cat. No.: HY-A0057A (Gypenoside VIII) Cat. No.: HY-N0043

Bioactivity: Gabapentin (Neurontin) is a pharmaceutical drug, specifically Bioactivity: Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional a GABA analog. It was originally developed to treat epilepsy, activity with an IC50 of 12.05±0.82 μM in HepG2 cells. and currently is also used to relieve neuropathic pain. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside… 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, 10 mg, 50 mg, 100 mg 5 mg, 10 mg

Ginsenoside Rf Ginsenoside Ro (Polysciasaponin P3; Chikusetsusaponin 5; (Panaxoside Rf) Cat. No.: HY-N0601 Chikusetsusaponin V) Cat. No.: HY-N0607

Bioactivity: Ginsenoside Rf is a trace component of root. Bioactivity: Ginsenoside Ro (Polysciasaponin P3; Chikusetsusaponin 5; Ginsenoside Rf inhibits N-type Ca2+ channel. Chikusetsusaponin V) exhibits a Ca2+-antagonistic antiplatelet

effect with an IC 50 of 155 μM. Ginsenoside Ro reduces the

production of TXA2 more than it reduces the activities… Purity: 94.90% Purity: 98.69% 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

GSK-7975A GV-58 Cat. No.: HY-12507 Cat. No.: HY-12498

Bioactivity: GSK-7975A is a potent and orally available CRAC channel Bioactivity: GV-58 is a potent, selective N- and P/Q-type Ca2+ channels inhibitor. agonist with EC50 of 7.21/8.81 uM for N-type/P-Q-type Ca2+ channel; 20-fold less potent CDK inhibitor activity.

Purity: 99.56% Purity: 99.09% 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 1 mg, 5 mg

Ibutilide fumarate Iganidipine (U70226E) Cat. No.: HY-B0387 Cat. No.: HY-101685

Bioactivity: Fumarate is a Class III that is Bioactivity: Iganidipine is a Ca2+ antagonist. indicated for acute cardioconversion of and atrial flutter of a recent onset to sinus rhythm.

Purity: 99.84% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 100 mg, 250 mg, 500 mg 10 mg, 50 mg, 100 mg

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Ionomycin (SQ23377) Cat. No.: HY-13434 (PN 200-110) Cat. No.: HY-B0233

Bioactivity: Ionomycin (SQ23377) is a Calcium ionophore and an antibiotic Bioactivity: Isradipine(Dynacirc) is a calcium channel blocker with an IC50 produced by Streptomyces conglobatus ATCC 31005. of 34±8 μM. Target: Calcium Channel Isradipine(Dynacirc) is a calcium channel blocker with an IC50 of 34±8 μM.It is usually prescribed for the treatment of high blood pressure in order to reduce the risk of stroke and heart attack[1]. Isradipine… Purity: 98.0% Purity: 99.24% Clinical Data: No Development Reported Clinical Data: Launched Size: 14.1 mM*500 μL in , Size: 10mM x 1mL in DMSO, 14.1 mM*100 μL in Ethanol, 10 mg, 50 mg, 100 mg

L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) Cat. No.: HY-N0215 Cat. No.: HY-B0347

Bioactivity: L-Phenylalanine is an antagonist at α2δ calcium channels with Bioactivity: Lacidipine (Lacipil, Motens) is a L-type calcium channel a Ki of 980 nM. blocker. Target: Calcium Channel Lacidipine, a novel third-generation dihydropyridine calcium channel blocker, has been demonstrated effective for hypertension. lacidipine protects HKCs against apoptosis induced by ATP depletion and… Purity: 98.06% Purity: 99.78% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 1 g 10 mg, 50 mg, 100 mg, 200 mg

Lemildipine (NB-818; NPK-1886) Cat. No.: HY-19663 Cat. No.: HY-B0612

Bioactivity: Lemildipine is a new dihydropyridine calcium entry blocker. Bioactivity: Lercanidipine is a calcium channel blocker of the dihydropyridine class.

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

Lercanidipine hydrochloride besylate Cat. No.: HY-B0612A ((S)-Amlodipine besylate; Levoamlodipine besylate) Cat. No.: HY-14744A

Bioactivity: Lercanidipine hydrochloride is a calcium channel blocker of Bioactivity: Levamlodipine besylate ((S)-Amlodipine besylate) is a powerful the dihydropyridine class. dihydropyridine calcium channel blocker, possessing properties and used in the treatment of hypertension and angina [1].

Purity: 98.50% Purity: 99.91% 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 10 mg, 50 mg

Lomerizine dihydrochloride (KB-2796) Cat. No.: HY-B0768A Cat. No.: HY-B0419

Bioactivity: dihydrochloride is an antagonist of L- and T-type Bioactivity: Manidipine is a calcium channel blocker that is used voltagegated calcium channels. clinically as an antihypertensive.

Purity: 99.97% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg, 200 mg 50 mg

www.MedChemExpress.com 15

Manidipine dihydrochloride McN5691 (CV-4093) Cat. No.: HY-17403 (RWJ26240) Cat. No.: HY-U00218

Bioactivity: Manidipine 2Hcl (CV-4093) is a dihydropyridine compound and a Bioactivity: McN5691 is a voltage-sensitive calcium channel blocker. calcium channel blocker for Ca2+ current with IC50 of 2.6 nM.

Purity: 99.18% 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 50 mg, 100 mg

Mibefradil dihydrochloride (Ro 40-5967) Cat. No.: HY-15553 (Ro 40-5967 (dihydrochloride)) Cat. No.: HY-15553A

Bioactivity: Mibefradil is a calcium channel blocker with moderate Bioactivity: Mibefradil dihydrochloride (Ro 40-5967 dihydrochloride) is a 2+ calcium channel blocker with moderate selectivity for T-type selectivity for T-type Ca channels displaying IC50s of 2.7 Ca 2+ channels displaying IC s of 2.7 μM and 18.6 μM for μM and 18.6 μM for T-type and L-type currents, respectively. 50 T-type and L-type currents, respectively. Purity: >98% Purity: 99.63% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

Mirogabalin besylate (DS5565) Cat. No.: HY-12650 (DS 5565 besylate) Cat. No.: HY-108006

Bioactivity: Mirogabalin (DS-5565) is a novel, preferentially selective Bioactivity: Mirogabalin besylate is a selective and orally available α2δ-1 ligand characterized by high potency and selectivity to ligand for the α2δ subunit of voltage-gated calcium channels,

the α2δ-1 subunit of voltage-sensitive calcium channel with Kds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human complexes in the CNS. α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively.

Purity: 99.31% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

ML218 MRS1845 Cat. No.: HY-103309 Cat. No.: HY-103310

Bioactivity: ML218 is a selective T-type calcium channel inhibitor with Bioactivity: MRS1845 is a Ca2+ channel blocker with relative specificity IC s of 270 and 310 nM for Cav3.3 and Cav3.2 in 50 for store-operated calcium entry (SOCE) channels [1]. electrophysiology assay, respectively.

Purity: 99.49% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg Size:

Myomodulin N-type calcium channel blocker-1 Cat. No.: HY-P0268 Cat. No.: HY-100310

Bioactivity: Myomodulin is a neuropeptide present in molluscs, insects, and Bioactivity: N-type calcium channel blocker-1 is an orally active analgesic gastropods. agent which shows high affinity to functionally block N-type

calcium channels with an IC50 of 0.7 μM in the IMR32 assay.

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

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

NecroX-5 sulfate Cat. No.: HY-104015 Cat. No.: HY-B0470

Bioactivity: NecroX-5 is a derivative of the NecroX, reduces intracellular Bioactivity: Neomycin sulfate is an aminoglycoside antibiotic used for calcium concentration, and possesses anti-inflammatory and preventing or treating bacterial infections. anti-cancer activity.

Purity: 99.31% 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, 25 mg, 50 mg, 100 mg 10 g, 25 g

Nexopamil racemate Cat. No.: HY-101727 (YC-93) Cat. No.: HY-12515

Bioactivity: Nexopamil racemate is the racemate of Nexopamil. Nexopamil is Bioactivity: Nicardipine(YC-93) is a calcium channel blocker that has been 2+ widely used to control blood pressure in severe hypertension a combined Ca / 5-HT2 antagonist on thrombus formation in following events such as ischemic stroke, traumatic brain vivo and on platelet aggregation in vitro. injury, and intracerebral hemorrhage.

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

Nicardipine Hydrochloride Nifedipine (YC-93 Hydrochloride) Cat. No.: HY-12515A (BAY-a-1040) Cat. No.: HY-B0284

Bioactivity: Nicardipine Hydrochloride (YC-93 Hydrochloride) is a calcium Bioactivity: Nifedipine (BAY-a-1040) is a potent calcium channel blocker channel blocker that has been widely used to control blood and drug of choice for cardiac insufficiencies. pressure in severe hypertension following events such as ischemic stroke, traumatic brain injury, and intracerebral hemorrhage. Purity: 99.85% Purity: 97.64% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 1 g, 5 g, 10 g

Nifedipine D6 (BAY-a-1040 D6) Cat. No.: HY-B0284S (FK235; FR34235) Cat. No.: HY-14284

Bioactivity: Nifedipine D6 (BAY-a-1040 D6) is deuterium labeled nifedipine, Bioactivity: Nilvadipine is a potent calcium channel antagonist, and the and nifedipine is a potent calcium channel blocker. IC50 value is around 0.1 nM.

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

Nimodipine (BAY-e 9736) Cat. No.: HY-B0265 (BAY-k 5552) Cat. No.: HY-17402

Bioactivity: (Nimotop) is a dihydropyridine derivative and an Bioactivity: Nisoldipine(BAY-k 5552; Sular) is a calcium channel blocker analogue of the calcium channel blocker nifedipine, with belonging to the dihydropyridines class, specific for L-type antihypertensive activity.Nimodipine decreases intracellular Cav1.2 with IC50 of 10 nM. IC50 value: 10 nM Target: L-type free Ca2+,Beclin-1 and autophagy. Target: Calcium Channel Cav1.2 Nisoldipine is a potent blocker of L-type calcium Nimodipine is main use is in the prevention of cerebral… channels. Nisoldipine binds directly to inactive calcium… Purity: 99.87% Purity: 98.22% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg, 500 mg, 1 g 100 mg, 500 mg

www.MedChemExpress.com 17

Nitrendipine NNC 55-0396 (BAY-E-5009) Cat. No.: HY-B0424 (NNC 55-0396 dihydrochloride) Cat. No.: HY-50722

Bioactivity: is a calcium channel blocker with marked Bioactivity: NNC 55-0396, Mibefradil derivative, is a highly selective vasodilator action. Target: Calcium Channel Nitrendipine is a T-type calcium channel blocker; displays IC50 values of 6.8 dihydropyridine calcium channel blocker. It is used in the and > 100 μM for inhibition of Cav3.1 T-type channels and treatment of primary hypertension to decrease blood pressure. HVA currents respectively in INS-1 cells. IC50 value: 6.8 nM Nitrendipine blocked Ca2+ currents very potently, with… Target: Cav3.1 T-type channel NNC 55-0396 can be an essential… Purity: 99.29% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 200 mg, 500 mg, 1 g 1 mg, 5 mg

Norverapamil hydrochloride NP118809 ((±)- hydrochloride; D591 hydrochlorid) Cat. No.: HY-100750 (39-1B4) Cat. No.: HY-14462

Bioactivity: Norverapamil hydrochloride is a calcium channel blocker it is Bioactivity: NP118809 is a potent N-type calcium channel blocker, with an the main active metabolite of . In vitro: IC50 of 0.11 μM; also less potently inhibits L-type calcium Norverapamil is similarly effective as verapamil at inhibiting channel with an IC of 12.2 μM. and rifampicin tolerance and killing of 50 intracellular M. tuberculosis in the absence of other .… Purity: 99.46% Purity: 98.62% 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, 10 mg, 25 mg 100 mg, 200 mg, 500 mg

NS-638 Palonidipine Cat. No.: HY-101428 Cat. No.: HY-108997

Bioactivity: NS-638 is a small nonpeptide molecule with Ca2+-channel Bioactivity: Palonidipine is a calcium antagonist which is potential for [1] [2] blocking properties. K +-stimulated intracellular Ca the therapy of angina-pectoris and hypertension 2+ [3]. -elevation is blocked with an IC50 value of 3.4 μM.

Purity: 98.04% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 100 mg, 500 mg, 250 mg 5 mg, 10 mg, 50 mg, 100 mg

PD0176078 PD173212 Cat. No.: HY-U00236 Cat. No.: HY-103318

Bioactivity: PD0176078 is a newly found N-type Calcium channel blocker. Bioactivity: PD173212 is a selective N-type voltage sensitive calcium

channel (VSCC) blocker, with an IC50 of 36 nM in IMR-32 assays.

Purity: >98% Purity: 95.65% 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

Penfluridol Pinaverium (R-16341) Cat. No.: HY-B1077 Cat. No.: HY-111613

Bioactivity: Penfluridol is a highly potent, first generation Bioactivity: is an L-type calcium channel blocker with diphenylbutylpiperidine antipsychotic. selectivity for the gastrointestinal tract, effectively relieves pain, diarrhea and intestinal discomfort, provides good therapeutic efficacies without significant adverse effects on Irritable bowel syndrome (IBS) patients [1]. Purity: 99.84% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg 50 mg

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

Ranolazine dihydrochloride (CVT 303; RS 43285-003) Cat. No.: HY-B0280 (CVT 303 (dihydrochloride); RS 43285) Cat. No.: HY-17401

Bioactivity: Ranolazine is an antianginal . Bioactivity: Ranolazine dihydrochloride (RS-43285) is an antianginal agent with antiarrhythmic properties that achieves its effects via a novel (inhibition of the late phase of the inward sodium current), without affecting heart rate or blood pressure (BP). IC50 value: Target: sodium-dependent calcium… Purity: 98.38% Purity: 99.92% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 100 mg, 200 mg, 500 mg 100 mg, 200 mg, 500 mg, 1 g, 5 g

Semotiadil recemate fumarate Sipatrigine Cat. No.: HY-U00026 (619C89; BW 619C89) Cat. No.: HY-108335

Bioactivity: Semotiadil recemate fumarate is the recemate of Semotiadil Bioactivity: Sipatrigine, a neuroprotective agent, is a glutamate release fumarate. Semotiadil fumarate is a novel vasoselective Ca2+ inhibitor, voltage-dependent and calcium channel antagonist. channel inhibitor, penetrating the central nervous system. Has potential to treat focal cerebral and stroke [1]

Purity: >98% Purity: 99.0% 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

SM-6586 SQ-31765 Cat. No.: HY-19062 (SQ31765; SQ 31765) Cat. No.: HY-101740

Bioactivity: SM-6586 is a calcium channel antagonist and inhibitor of Na Bioactivity: SQ-31765 is a benzazepine calcium channel blocker. +/H + and Na+/Ca2+ exchange transport, potentially for the treatment of cerebrovasular diseases and hypertension.

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

TDN345 Teludipine hydrochloride Cat. No.: HY-101669 (GR53992B; GX1296B ) Cat. No.: HY-101621

Bioactivity: TDN345 is a Ca2+ antagonist, used for the treatment of Bioactivity: Teludipine is a lipophilic calcium channel blocker. vascular and senile dementia including 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

Tetracaine hydrochloride (Amethocaine hydrochloride) Cat. No.: HY-B0473 (NSC-77037d-Tetrandrine) Cat. No.: HY-13764

Bioactivity: HCl is a potent local anaesthetic and a channel Bioactivity: Tetrandrine (NSC-77037) is a bis-benzyl-isoquinoline , function allosteric inhibitor. which inhibits voltage-gated Ca2+ current (ICa) and Ca 2+-activated K+ current.

Purity: 99.97% Purity: 99.90% Clinical Data: Launched Clinical Data: Launched Size: 100 mg Size: 100 mg, 250 mg

www.MedChemExpress.com 19

Thapsigargin Tiapamil hydrochloride (Thapsigargin (TG)) Cat. No.: HY-13433 (Ro 11-1781) Cat. No.: HY-101674

Bioactivity: Thapsigargin is an inhibitor of microsomal Ca2+-ATPase. Bioactivity: Tiapamil hydrochloride is a calcium channel blocker.

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 1 mg, 5 mg

Trimethadione TTA-Q6 (3,5,5,-Trimethyloxazolidine-2,4-dione) Cat. No.: HY-A0092 Cat. No.: HY-10388

Bioactivity: is an anticonvulsant; commonly Bioactivity: TTA-Q6 is a selective T-type Ca2+ channel antagonist, used in used to treat epileptic conditions. the neurological disease.

Purity: 98.0% Purity: 99.94% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg 5 mg, 10 mg, 25 mg, 50 mg

UK51656 Verapamil hydrochloride Cat. No.: HY-101707 ((±)-Verapamil hydrochlorid) Cat. No.: HY-A0064

Bioactivity: UK51656 is a calcium antagonist with IC50 of 4 nM. Bioactivity: Verapamil hydrochloride is a calcium channel antagonist.

Purity: >98% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 1 g, 5 g

YS-201 Cat. No.: HY-U00137 (AD 810; CI 912) Cat. No.: HY-B0124

Bioactivity: YS-201 is a dihydropyridine-type calcium channel antagonist Bioactivity: Zonisamide is a 1,2 benzisoxazole derivative and the first previously in clinical trials for the treatment of angina agent of this chemical class to be developed as an pectoris and hypertension. antiepileptic drug.

Purity: 99.0% Purity: 99.72% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 200 mg, 500 mg

Zonisamide sodium ZSET1446 (AD 810 sodium; CI 912 sodium) Cat. No.: HY-B0124A (ST-101) Cat. No.: HY-11013

Bioactivity: Zonisamide sodium is a 1,2 benzisoxazole derivative and the Bioactivity: ZSET1446 is a novel cognitive enhancer that significantly first agent of this chemical class to be developed as an improves learning deficits in various types of Alzheimer antiepileptic drug. disease (AD) models.

Purity: >98% Purity: 98.03% Clinical Data: Launched Clinical Data: Phase 2 Size: 200 mg, 500 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

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

β-Amino Acid Imagabalin Hydrochloride (PD-0332334) Cat. No.: HY-U00250

Bioactivity: β-Amino Acid Imagabalin Hydrochloride (PD-0332334) is a ligand for the α2δ subunit of the voltage-dependent calcium channel.

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

www.MedChemExpress.com 21 CFTR transmembrane conductance regulator

CFTR (Cystic fibrosis transmembrane conductance regulator) is a membrane protein in vertebrates that is encoded by the CFTR gene. CFTR is an ABC transporter-class ion channel that conducts chloride and thiocyanate ions across epithelial cell membranes. Mutations of the CFTR gene affecting chloride ion channel function lead to dysregulation of epithelial fluid transport in the lung, pancreas and other organs, resulting in cystic fibrosis. Complications include thickened mucus in the lungs with frequent respiratory infections, and pancreatic insufficiency giving rise to malnutrition and diabetes. These conditions lead to chronic disability and reduced life expectancy. CFTR functions as a cAMP-activated ATP-gated anion channel, increasing the conductance for certain anions to flow down their electrochemical gradient. ATP-driven conformational changes in CFTR open and close a gate to allow transmembrane flow of anions down their electrochemical gradient. CFTR is an ion channel that evolved as a 'broken' ABC transporter that leaks when in open conformation.

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

(R)-BPO-27 Ataluren Cat. No.: HY-19778 (PTC124) Cat. No.: HY-14832

Bioactivity: (R)-BPO-27 is a potent CFTR inhibitor with an IC50 of 4 nM. Bioactivity: Ataluren (PTC124) is an orally available CFTR-G542X nonsense allele inhibitor.

Purity: 99.56% Purity: 99.88% 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 10 mg, 50 mg, 100 mg, 200 mg

BPO-27 racemate CFTR corrector 1 Cat. No.: HY-19778A Cat. No.: HY-111772

Bioactivity: BPO-27 racemate is a potent CFTR inhibitor with an IC50 of 8 Bioactivity: CFTR corrector 1 (compound 1) is a modulator of cystic fibrosis nM. transmembrane conductance regulator (CFTR). CFTR corrector 1 (compound 1) facilitates the processing and trafficking of CFTR to increase the amount of CFTR at the cell surface [1].

Purity: 98.67% 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, 50 mg, 100 mg

CFTR corrector 2 CFTR(inh)-172 Cat. No.: HY-125381 Cat. No.: HY-16671

Bioactivity: CFTR corrector 2 is a cystic fibrosis transmembrane conductance Bioactivity: CFTR(inh)-172 is a potent and selective blocker of the CFTR corrector (CFTR), extracted from patent US20140274933 [1]. chloride channel; reversibly inhibits CFTR short-circuit current in less than 2 minutes with a Ki of 300 nM.

Purity: >98% Purity: 98.82% 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

GLPG1837 GLPG2451 (ABBV-974) Cat. No.: HY-111099 Cat. No.: HY-119936

Bioactivity: GLPG1837 is a potent and reversible CFTR potentiator, with Bioactivity: GLPG2451 is a cystic fibrosis transmembrane conductance

EC50s of 3 nM and 339 nM for F508del and G551D CFTR, regulator (CFTR) potentiator, which effectively potentiates low temperature rescued F508del CFTR with an EC of 11.1 nM respectively. 50 [1]. Purity: 99.15% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 100 mg, 250 mg, 500 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

GlyH-101 IOWH-032 Cat. No.: HY-18336 Cat. No.: HY-18337

Bioactivity: GlyH-101 is a cell-permeable glycinyl compound that Bioactivity: IOWH-032 is a novel and potent CFTR inhibitor (IC50=1.01 uM) blocks CFTR with Ki of 1.4 uM. in T84 and CHO-CFTR cell based assays. IC50 value: 1.01 uM (CHO-CFTR FLIPR) [1] Target: CFTR Profiling of iOWH032 showed it to be a CFTR inhibitor in T84 and CHO-CFTR cell based assays. It also demonstrated statistical significant… Purity: 99.35% Purity: 99.66% 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 10 mg, 50 mg

www.MedChemExpress.com 23

Ivacaftor benzenesulfonate (VX-770) Cat. No.: HY-13017 (VX-770 benzenesulfonate) Cat. No.: HY-13017A

Bioactivity: Ivacaftor is a potent and orally bioavailable CFTR Bioactivity: Ivacaftor benzenesulfonate is an orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with potentiator, used for cystic fibrosis treatment.

EC50s of 100 nM and 25 nM, respectively.

Purity: 99.93% Purity: >98% 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, 100 mg

Ivacaftor hydrate KM11060 (VX-770 hydrate) Cat. No.: HY-13017B Cat. No.: HY-19970

Bioactivity: Ivacaftor hydrate is an orally bioavailable CFTR potentiator, Bioactivity: KM11060 is a novel corrector of the F508del-CFTR trafficking used for cystic fibrosis treatment. defect.

Purity: >98% Purity: 99.80% Clinical Data: Launched Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg

Lumacaftor PPQ-102 (VX-809; VRT 826809) Cat. No.: HY-13262 (CFTR Inhibitor) Cat. No.: HY-14179

Bioactivity: Lumacaftor (VX-809) is a CFTR modulator that corrects the Bioactivity: PPQ-102 is a potent CFTR inhibitor which can completely folding and trafficking of CFTR protein. inhibited CFTR chloride current with IC 50approximately 90 nM.

Purity: 99.12% Purity: 98.19% 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

PTI-428 Tezacaftor Cat. No.: HY-111680 (VX-661) Cat. No.: HY-15448

Bioactivity: PTI-428 is a specific cystic fibrosis transmembrane Bioactivity: Tezacaftor (VX-661) is a second F508del CFTR corrector and conductance regulator ( CFTR) amplifier [1]. help CFTR protein reach the cell surface.

Purity: 99.77% Purity: 99.92% 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, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

24 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Chloride Channel Cl− Channels

Chloride channels represent a relatively under-explored target class for drug discovery as elucidation of their identity and physiological roles has lagged behind that of many other drug targets. Chloride channels are involved in a wide range of biological functions, including epithelial fluid secretion, cell-volume regulation, neuroexcitation, smooth-muscle contraction and acidification of intracellular organelles. Mutations in several chloride channels cause human diseases, including cystic fibrosis, macular degeneration, myotonia, stones, renal salt wasting and hyperekplexia. Chloride-channel modulators have potential applications in the treatment of some of these disorders, as well as in secretory diarrhoeas, polycystic kidney disease, osteoporosis and hypertension. Chloride channel accessory proteins, also known as calcium-activated chloride channel regulators (CLCA proteins), are a family of transmembrane proteins that have been suggested to have a role in chloride conductance in epithelial cells.

www.MedChemExpress.com 25 Chloride Channel Inhibitors & Modulators

Adjudin CaCCinh-A01 (AF-2364) Cat. No.: HY-18996 Cat. No.: HY-100611

Bioactivity: Adjudin is an extensively studied with a Bioactivity: CaCCinh-A01 is an inhibitor of both TMEM16A and superior mitochondria-inhibitory effect. Adjudin is also a calcium-activated chloride channel ( CaCC) with IC50s of - potent Cl channel blocker. 2.1 and 10 μM, respectively.

Purity: 98.0% Purity: 99.60% 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

Chlorotoxin DCPIB Cat. No.: HY-P0173A Cat. No.: HY-103371

Bioactivity: Chlorotoxin is a 36 amino-acid peptide from the venom of the Bioactivity: DCPIB is a selective, reversible and potent inhibitor of Israeli scorpion Leiurus quinquestriatus with anticancer volume-regulated anion channels ( VRAC), voltage-dependently activity. Chlorotoxin is a . activates potassium channels TREK1 and TRAAK, inhibits TRESK,

TASK1 and TASK3 ( IC50s, 0.14, 0.95, 50.72 μM, respective…

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

Endovion Flufenamic acid (NS3728) Cat. No.: HY-105917 Cat. No.: HY-B1221

Bioactivity: Endovion (NS3728) is a pharmacological anion channel inhibitor Bioactivity: Flufenamic acid is a non-steroidal anti-inflammatory agent, (like chloride channel) and the specific VRAC/VSOAC blocker. inhibits cyclooxygenase ( COX), activates AMPK, and also Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel modulates ion channels, blocking chloride channels and L-type inhibitor [1] [2]. Ca2+ channels, modulating non-selective cation channel…

Purity: 99.27% Purity: 99.92% Clinical Data: No Development Reported Clinical Data: Launched Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 100 mg

H100 Lubiprostone Cat. No.: HY-100322 (RU-0211; SPI-0211) Cat. No.: HY-B0679

Bioactivity: H100 is a Cl- transport inhibitor, with partial effects Bioactivity: Lubiprostone(SPI-0211;RU0211) is a gastrointestinal agent used against both the NaK2Cl cotransporter and the Band 3 anion for the treatment of idiopathic chronic constipation. exchanger, but no effect against KCl cotransporter, in human erythrocytes.

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 DMSO, 1 mg, 5 mg, 10 mg, 50 mg

Meticrane Cat. No.: HY-B0908 Cat. No.: HY-B0493

Bioactivity: is a . Meticrane inhibits the reabsorption Bioactivity: Niflumic acid, a Ca2+-activated Cl- channel blocker, is an of sodium and chloride ions in the . analgesic and anti-inflammatory agent used in the treatment of Meticrane is used to treat essential hypertension. rheumatoid arthritis.

Purity: 98.79% Purity: 99.86% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 100 mg

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

NPPB (5-Nitro-2-(3-phenylpropylamino); Hoechst NS1652 144; HOE 144) Cat. No.: HY-101012 Cat. No.: HY-100244

Bioactivity: NPPB is a blocker of the outwardly rectifying chloride Bioactivity: NS1652 is a reversible anion conductance inhibitor, blocks

channel ( ORCC). chloride channel, with an IC50 of 1.6 μM in human and mouse red blood cells.

Purity: 99.89% 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 10 mg, 50 mg, 100 mg

R(+)-IAA-94 Shikonin (R(+)-Methylindazone) Cat. No.: HY-12693 (C.I. 75535; Isoarnebin 4) Cat. No.: HY-N0822

Bioactivity: R(+)-IAA-94 is a potent indanyloxyacetic acid blocker of Bioactivity: Shikonin is a major component of a Chinese herbal medicine epithelial chloride channels. named zicao. Shikonin has shown various biological activities, including inhibition of TNF-α, NF-κB, HIV-1.

Purity: 99.70% Purity: 99.80% 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 10 mg, 25 mg, 50 mg, 100 mg

T16Ainh-A01 Cat. No.: HY-100612

Bioactivity: T16Ainh-A01, an aminophenylthiazole, is a potent transmembrane protein 16A (TMEM16A) inhibitor,

inhibiting TMEM16A-mediated chloride currents with an IC50 value of ~1 µM. TMEM16A (ANO1) functions a…

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

www.MedChemExpress.com 27 CRAC Channel Calcium release-activated channels;Ca2+ release-activated Ca2+ channels

The Ca2+ release-activated Ca2+ (CRAC) channel is a highly Ca2+ -selective store-operated channel expressed in T cells, mast cells, and various other tissues. CRAC channels regulate critical cellular processes such as gene expression, motility, and the secretion of inflammatory mediators. The identification of Orai1, a key subunit of the CRAC channel pore, and STIM1, the endoplasmic reticulum (ER) Ca2+ sensor, have provided the tools to illuminate the mechanisms of regulation and the pore properties of CRAC channels. Opening of CRAC channels enables the refilling of ER Ca2+ stores and sustains long-lasting Ca2+ oscillations and plateau signals, critical for the proliferation of T cells and production of cytokines following antigenic stimulation.

28 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] CRAC Channel Inhibitors & Modulators

CM-4620 CRAC intermediate 1 Cat. No.: HY-101942 Cat. No.: HY-20587

Bioactivity: CM-4620 is a calcium-release activated calcium-channel (CRAC) Bioactivity: CRAC intermediate 1 is a key intermediate in the chemical synthesis of a series of CRAC channel inhibitors, detailed inhibitor, with IC50s of 119, 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively. information can be found in Patent WO 2010122089 A1, intermediate 9.

Purity: 99.94% 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 5 mg, 10 mg

CRAC intermediate 2 GSK-5498A Cat. No.: HY-20588 Cat. No.: HY-12521

Bioactivity: CRAC intermediate 2 is a intermediate compound for CRAC Bioactivity: GSK-5498A is a selective small molecule blocker of CARC ( inhibitor synthesis, extracted from patent WO 2013059666A1. IC50, 1 μM); inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.

Purity: 99.96% Purity: 97.45% 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

SOCE inhibitor 1 Synta66 Cat. No.: HY-112913 Cat. No.: HY-111325

Bioactivity: SOCE inhibitor 1 is a store-operated calcium entry (SOCE) Bioactivity: Synta66 is an inhibitor of store-operated calcium entry channel Orai, which forms the pore of the CRAC channel, and inhibitor with an IC50 of 4.4 μM. used for the research of neurological disease.

Purity: >98% Purity: 99.31% 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, 25 mg

YM-58483 (BTP2) Cat. No.: HY-100831

Bioactivity: YM-58483 is the first selective and potent inhibitor of CRAC channels and subsequent Ca 2+ signals.

Purity: 98.77% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

www.MedChemExpress.com 29 CRM1 Chromosomal Maintenance 1;Exportin 1;XPO1

Chromosome maintenance protein 1 (CRM1) is a nuclear export receptor involved in the active transport of tumor suppressors (eg, p53 and nucleophosmin) whose function is altered in cancer because of increased expression and overactive transport. Blocking CRM1-mediated nuclear export of such proteins is a novel therapeutic strategy to restore tumor suppressor function. Orally bioavailable selective inhibitors of nuclear export (SINE) that irreversibly bind to CRM1 and block the function of this protein have been recently developed. CRM1 is the sole exporter of many tumor-suppressor proteins (TSPs), and functions as a proto-oncogene by transporting these tumor suppressors from the nucleus, where they are active, to the cytoplasm, where their activity is abrogated.

30 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] CRM1 Inhibitors & Modulators

CBS9106 Eltanexor Z-isomer (SL-801) Cat. No.: HY-108716 (KPT-8602 (Z-isomer)) Cat. No.: HY-100423A

Bioactivity: CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with Bioactivity: Eltanexor Z-isomer (KPT-8602 Z-isomer) is the less active CRM1 degrading and antitumor activities [1]. isomer of KPT-8602. KPT-8602 is a potent CRM1 inhibitor. IC50 In Vitro: Eltanexor Z-isomer exhibits different

inhibitory effects on Z138, MM15, 3T3 cell lines, with IC 50

Purity: >98% Purity: 95.80% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg

Leptomycin B (CI 940; LMB) Cat. No.: HY-16909

Bioactivity: Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/ exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle [1]. Purity: 98.0% Clinical Data: No Development Reported Size: 0.046 mM * 200 uL in Ethanol ,

www.MedChemExpress.com 31 EAAT2 Excitatory amino acid transporter 2;Glutamate transporter 1;GLT-1

Excitatory amino acid transporter 2 (EAAT2) is the major glutamate transporter and functions to remove glutamate from synapses. An increase in EAAT2 protein expression and function may provide a means to prevent insufficient glutamate and consequently reduce neuronal damage. The glial glutamate transporter EAAT2 plays a major role in glutamate clearance. EAAT2 can be upregulated by transcriptional or translational activation.EAAT2 is a potential target for the prevention of excitotoxicity.

32 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] EAAT2 Inhibitors & Modulators

GT 949 LDN-212320 Cat. No.: HY-114381 (LDN/OSU-0212320; LDN-0212320; OSU-0212320) Cat. No.: HY-12741

Bioactivity: GT 949 is a selective excitatory amino acid transporter-2 ( Bioactivity: LDN-212320(OSU-0212320) is a glutamate transporter EAAT2

EAAT2) positive with an EC50 of 0.26 activator; enhances EAAT2 levels by > 6 fold at concentrations < 5 μM after 24 h. nM [1].

Purity: >98% Purity: 96.72% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

WAY-213613 Cat. No.: HY-107523

Bioactivity: WAY-213613 is a potent, selective human EAAT2 inhibitor (

IC50, 85 nM), exhibits 59- and 45-fold selectivity over human EAAT1 and EAAT3. Inhibits glutamate uptake in rat cortical synaptosomes [1]. Purity: 99.0% Clinical Data: No Development Reported Size: 5 mg

www.MedChemExpress.com 33 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.

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

(+)-Kavain (-)-Borneol Cat. No.: HY-B1671 (L-Borneol) Cat. No.: HY-N1368B

Bioactivity: (+)-Kavain, a main kavalactone 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)-Baclofen 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. . 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

www.MedChemExpress.com 35

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 consumption in animal models of alcohol addiction. IC50 value: Target: GABA receptor Acamprosate, or N-acetyl , 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 -like activity in mice. receptor. Used to treat postpartum depression.

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-butyric acid (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

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

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 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 ion channel. Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg Size: 1 mg, 5 mg

www.MedChemExpress.com 37

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 chloride channel displays anxiogenic and potent convulsant 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

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

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 Guvacine 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

www.MedChemExpress.com 39

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

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

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, , and monoaminergic

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

www.MedChemExpress.com 41

Primidone Cat. No.: HY-B0339 Cat. No.: HY-B0546

Bioactivity: is an anticonvulsant of the pyrimidinedione class. Bioactivity: Procaine is a local drug of the amino group, which acts through multiple targets. Target: Others Procaine is a 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: Remimazolam benzenesulfonate is a GABA agonist. Bioactivity: Rilmazafone is a benzodiazepine ω ligand with 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

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

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, , 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

www.MedChemExpress.com 43

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 placebo 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

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

www.MedChemExpress.com 45 GlyT Inhibitors & Modulators

Bitopertin 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

46 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] HCN Channel Hyperpolarization activated cyclic nucleotide gated channels

Hyperpolarization- and Cyclic Nucleotide-gated (HCN) channels are a family of six transmembrane domain, single pore-loop, hyperpolarization activated, non-selective cation channels. The HCN family consists of four members (HCN1-4). HCN channels represent the molecular correlates of I(h), a hyperpolarization-activated current best known for its role in controlling heart rate and in the regulation of neuronal resting membrane potential and excitability. HCN channels are unique among vertebrate voltage-gated ion channels, in that they have a reverse voltage-dependence that leads to activation upon hyperpolarization. HCN channels are encoded by four genes (HCN1-4) and are widely expressed throughout the heart and the central nervous system.

www.MedChemExpress.com 47 HCN Channel Inhibitors & Modulators

Cilobradine hydrochloride Zatebradine (DK-AH 269) Cat. No.: HY-18940A (UL-FS-49 (free base); UL-FS-49CL (free base)) Cat. No.: HY-13422A

Bioactivity: Cilobradine is an HCN Channel blocker; an open channel blocker Bioactivity: Zatebradine(UL-FS-49 free base; UL-FS-49CL free base) is a of neuronal Ih and related cardiac If channels. Target: HCN potent HCN channels antagonist, which decreased the heartbeat Channel blocker Cilobradine is a HCN channel blocker that is in a reversible manner; 92% inhibition of the hHCN1-mediated about 3 times more potent than ZD7288. At a concentration of current at 10 uM. IC50 value: 10 uM(92% 92% inhibition of the 10 μM, Cilobradine inhibits WT mHCN2 channel current by 86 ±… hHCN1) [1] Target: hHCN channel antagonist The pharmacological… Purity: >98% Purity: 98.80% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 2 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

Zatebradine hydrochloride ZD7288 (UL-FS-49; UL-FS-49CL) Cat. No.: HY-13422 (ICI D7288) Cat. No.: HY-101346

Bioactivity: Zatebradine hydrochloride (UL-FS-49; UL-FS-49CL) is a potent Bioactivity: ZD7288 is a selective hyperpolarization-activated cyclic HCN channels antagonist, which decreased the heartbeat in a nucleotide-gated ( HCN) channel blocker. reversible manner; 92% inhibition of the hHCN1-mediated current at 10 uM. IC50 value: 10 uM(92% 92% inhibition of the hHCN1) [1] Target: hHCN channel antagonist The pharmacological… Purity: 99.15% Purity: 99.79% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in Water, 5 mg, 10 mg, 50 mg 5 mg, 10 mg

48 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] 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 ions to depolarise the postsynaptic membrane. NMDA receptors are blocked by 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.

www.MedChemExpress.com 49 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 -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

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

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

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CNS-5161 hydrochloride Coluracetam (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 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 Dynorphin A 1-10 Cat. No.: HY-P1594A Cat. No.: HY-P1594

Bioactivity: Dynorphin A (1-10) (TFA), an endogenous 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

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

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 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

www.MedChemExpress.com 53

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 acetylcholine receptor. 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

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

Linalool LY450108 Cat. No.: HY-N0368 Cat. No.: HY-10935

Bioactivity: 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: Meclofenoxate hydrochloride, an ester of dimethylethanolamine 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: Mephenesin 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 toxin, 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

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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-.

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- 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

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

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 Procyclidine 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 neuropathic pain 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

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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 Sunifiram 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 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

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

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

www.MedChemExpress.com 59

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

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

Monoamine transporters (MATs) are protein structures that function as integral plasma-membrane transporters to regulate concentrations of extracellular monoamine . Three major classes of MATs (SERT, DAT, NET) are responsible for the reuptake of their associated amine neurotransmitters (serotonin, dopamine, norepinephrine). MATs are located just outside the synaptic cleft (peri-synaptically), transporting monoamine transmitter overflow from the synaptic cleft back to the cytoplasm of the pre-synaptic neuron. MAT regulation generally occurs throughphosphorylation and posttranslational modification. Due to their significance in neuronal signaling, MATs are commonly associated with drugs used to treat mental disorders as well as recreational drugs. Compounds targeting MATs range from such as the wide variety of , selective serotonin reuptake inhibitors to stimulantmedications and amphetamine.

www.MedChemExpress.com 61 Monoamine Transporter Inhibitors & Modulators

(+)-Tetrabenazine D6 NBI-98782 Cat. No.: HY-B0590S1 ((+)-DTBZ; (+)-α-Dihydrotetrabenazine; (+)-α-DHTBZ) Cat. No.: HY-15793

Bioactivity: (+)-Tetrabenazine D6 is the deuterium labeled Bioactivity: NBI-98782(alpha-dihydrotetrabenazine) is a vesicular monoamine (+)-Tetrabenazine. (+)-Tetrabenazine is a reversible inhibitor transporter (VMAT2) inhibtior with an Ki value of 0.97 nM. of vesicular monoamine transporter 2 (VMAT-2).

Purity: >98% Purity: 99.80% 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

Radafaxine hydrochloride (GW-353162A; BW-306U) Cat. No.: HY-17590 Cat. No.: HY-N0480

Bioactivity: Radafaxine Hcl(BW-306U; GW-353162A) is a potent metabolite of Bioactivity: Reserpine is an inhibitor of the vesicular monoamine ; selective for inhibiting the reuptake of transporter 2 ( VMAT2). norepinephrine over dopamine; DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, and nAChR family modulator. Purity: 99.47% Purity: 99.83% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 100 mg

Reserpine hydrochloride Tetrabenazine Cat. No.: HY-N0480A (Ro 1-9569) Cat. No.: HY-B0590

Bioactivity: Reserpine hydrochloride is an inhibitor of the vesicular Bioactivity: Tetrabenazine is a VMAT-inhibitor used for treatment of monoamine transporter 2 ( VMAT2). hyperkinetic movement disorder. Target: Others tetrabenazine (TBZ), a monoamine-depleting and a dopamine-receptor-blocking drug. TBZ is an effective and safe drug for the treatment of a variety of hyperkinetic movement disorders. In contrast to… Purity: 99.84% Purity: 99.10% 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, 200 mg

Tetrabenazine ((+)-) ((+)-Tetrabenazine; (+)-TBZ; Tetrabenazine D6 (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine) Cat. No.: HY-B0590B (Ro 1-9569 D6) Cat. No.: HY-B0590S

Bioactivity: Tetrabenazine ((+)-) is a reversible inhibitor of vesicular Bioactivity: Tetrabenazine D6 is the deuterium labeled Tetrabenazine, which monoamine transporter 2 (VMAT-2), inhibits transport by VMAT2 is a VMAT-inhibitor used for treatment of hyperkinetic with 10-fold greater potency than transport by VMAT1. target: movement disorder. VMAT-2 In vitro: Tetrabenazine ((+)-) inhibit the activity of the transporter but appear to interact differently with the… Purity: 99.81% Purity: 99.0% 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

Tetrabenazine Racemate Trans (2,3)-Dihydrotetrabenazine (Ro 1-9569 Racemate) Cat. No.: HY-B0590A ((2R,3R,11bR)-rel-Dihydrotetrabenazine; …) Cat. No.: HY-15793A

Bioactivity: Tetrabenazine (Racemate) is a selective and reversible Bioactivity: Trans (2,3)-Dihydrotetrabenazine, a metabolite of inhibitor of vesicular monoamine transporter-2 (VMAT-2). Tetrabenazine, shows remarkable inhibition activity on vesicular monoamine transporter (VMAT2) [1].

Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

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

Vanilpyruvic acid (Vanylpyruvic acid) Cat. No.: HY-101416

Bioactivity: Vanilpyruvic acid is a catecholamine metabolite and precursor to vanillactic acid.

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

www.MedChemExpress.com 63 Monocarboxylate Transporter

Monocarboxylate transporters (MCTs) constitute a family of proton-linked plasma membrane transporters that carry molecules having one carboxylate group (monocarboxylates), such aslactate and pyruvate, across biological membranes. Highly malignant tumors rely heavily on aerobic glycolysis (metabolism of glucose to lactic acid even under ample tissue oxygen; Warburg Effect) and thus need to efflux lactic acid via MCTs to the tumor micro-environment to maintain a robust glycolytic flux and to prevent the tumor from being "pickled to death". The MCTs have been successfully targeted in pre-clinical studies using RNAi and a small-molecule inhibitor alpha-cyano-4-hydroxycinnamic acid (ACCA; CHC) to show that inhibiting lactic acid efflux is a very effective therapeutic strategy against highly glycolytic malignant tumors.

64 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Monocarboxylate Transporter Inhibitors & Modulators

7ACC1 7ACC2 (DEAC; Coumarin D 1421; D 1421) Cat. No.: HY-D0067 Cat. No.: HY-D0713

Bioactivity: 7ACC1(DEAC; Coumarin D 1421; D 1421) selectively interfere Bioactivity: 7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for with lactate fluxes in the lactate-rich tumor inhibition of [14C]-lactate influx; new antitumor treatment microenvironment; inhibits lactate influx but not efflux in targeting lactate transport in cancer cells. IC50 value: 11 nM tumor cells expressing MCT1 and MCT4 transporters. IC50 value: ([14C]-lactate influx) [1] Target: MCT inhibitor; lactate 0.86 uM(Lactate uptake inhibition) [1] Target: MCT inhibitor;… transport inhibitor 7ACC2 did not influence the prothrombin… Purity: 99.66% Purity: 99.44% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 200 mg 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

AR-C155858 AZD3965 Cat. No.: HY-13248 Cat. No.: HY-12750

Bioactivity: AR-C155858 is a selective monocarboxylate transporter MCT1 Bioactivity: AZD3965 is a selective MCT1 inhibitor with a Ki of 1.6 nM, and MCT2 inhibitor with K s of 2.3 nM and 10 nM, i showing 6-fold selectivity over MCT2. respectively.

Purity: 95.0% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

BAY-8002 Cat. No.: HY-122312

Bioactivity: BAY-8002 is a potent, selective, orally active inhibitor of

monocarboxylate transporter 1 (MCT1), with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4. Anti-tumor activity [1]. Purity: 98.10% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 65 Na+/Ca2+ Exchanger

Na +/Ca 2+ exchanger (sodium-calcium exchanger , NCX) is an antiporter membrane protein that removes calcium from cells. It uses the energy that is stored in the electrochemical gradient of sodium (Na +) by allowing Na + to flow down its gradient across the plasma membrane in exchange for the countertransport of calcium ions (Ca 2+). Na +/Ca 2+ exchanger removes a single calcium ion in exchange for the import of three sodium ions. Na +/Ca 2+ exchanger exists in many different cell types and animal species. Na +/Ca 2+ exchanger is considered one of the most important cellular mechanisms for removing Ca 2+. The Na +/Ca 2+ exchanger does not bind very tightly to Ca 2+ (has a low affinity), but it can transport the ions rapidly (has a high capacity), transporting up to five thousand Ca 2+ ions per second. The Na +/Ca 2+ exchanger also likely plays an important role in regaining the cell's normal calcium concentrations after an excitotoxic insult.

66 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Na+/Ca2+ Exchanger Inhibitors & Modulators

Caldaret CGP37157 (MCC-135) Cat. No.: HY-100298 Cat. No.: HY-15754

Bioactivity: Caldaret is an intracellular Ca2+ handling modulator that Bioactivity: CGP37157 is a potent, selective inhibitor of Na+/Ca2+ acts through reverse mode Na+/ Ca2+ exchanger inhibition. exchanger, inhibiting the Na +-induced Ca 2+-release from

guinea-pig heart mitochondria, with an IC50 of 0.8 μM.

Purity: >98% Purity: 99.79% 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

KB-R7943 mesylate ORM-10103 Cat. No.: HY-15415 Cat. No.: HY-128678

Bioactivity: KB-R7943 mesylate is a widely used inhibitor of the reverse Bioactivity: ORM-10103 is a specific inhibitor of the Na+/Ca2+ exchanger + 2+ (NCX), which decreases the NCX current with estimated IC s Na /Ca exchanger (NCX rev) with IC50 of 5.7±2.1 µM. 50 of 55 and 67 nM at -80 and at 20 mV, respectively [1] [2].

Purity: 99.39% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg 10 mg, 50 mg

ORM-10962 SEA0400 Cat. No.: HY-123785 Cat. No.: HY-15515

Bioactivity: ORM-10962 is a potent, highly selective sodium-calcium Bioactivity: SEA0400 is a novel and selective inhibitor of the Na +-Ca 2+ exchanger (NCX) inhibitor, with IC values of 67 and 55 nM 50 exchanger ( NCX), inhibiting Na +-dependent Ca 2+ uptake in [1] for the reverse and forward mode inhibition, respectively cultured neurons, astrocytes, and microglia with IC50s of from [2]. 5 to 33 nM. Purity: >98% Purity: 99.97% 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, 50 mg

SM-6586 SN 6 Cat. No.: HY-19062 Cat. No.: HY-107658

Bioactivity: SM-6586 is a calcium channel antagonist and inhibitor of Na Bioactivity: SN 6 is a selective Na+/Ca2+ exchanger (NCX) inhibitor, + + + 2+ /H and Na /Ca exchange transport, potentially for and inhibits 45Ca 2+ uptake by NCX1, NCX2, and NCX3, with the treatment of cerebrovasular diseases and hypertension. IC50s of 2.9, 16, and 8.6 μM, respectively.

Purity: >98% Purity: 99.0% 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

www.MedChemExpress.com 67 Na+/HCO3- Cotransporter Na/HCO3 cotransporter;NBC

The electrogenic Na/HCO3 cotransporter (symporter) is the major HCO3- transporter of the renal (PiT), located at the basolateral membrane (BLM), and also plays a noteworthy role in Na+ reabsorption. HCO3 transporters are important for regulation of intracellular pH (pHi) in most cells and also thereby regulate blood pH. This electrogenic Na/HCO3 cotransporter is first discovered using perfused Ambystoma tigrinum (salamander) renal, proximal tubules. This novel cotransporter mediates the movement of one Na+ ion with several HCO3- ions, making it electrogenic, is blocked by stilbene compounds, but does not depend on intra- or extracellular Cl-. This and similar cotransporters have been found in a number of tissues and cell types.

68 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Na+/HCO3- Cotransporter Inhibitors & Modulators

S0859 Cat. No.: HY-15529

Bioactivity: S0859, an N-cyanosulphonamide compound, reversibly inhibit NBC-mediated pH(i) recovery (K (i)=1.7 microM, full inhibition at approximately 30 microM). IC50 value: Target: NBC Na(+)-coupled HCO(3)(-) transporters (NBCs) mediate the transport of bicarbonate ions across cell membranes and are… Purity: 99.78% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

www.MedChemExpress.com 69 Na+/K+ ATPase Sodium potassium pump

Na+/K+ ATPase (Sodium potassium pump) is a transmembrane protein complex found in all higher eukaryotes acting as a key energy-consuming pump maintaining ionic and osmotic balance in cells. Na+/K+ ATPase is an emerging cancer target that merits further investigation. The constant activity of the Na+/K+-ATPase (NKA, or Na+ pump) is essential for re-establishing and maintaining this gradient. In cardiac and vascular smooth muscle the principal isoforms of the NKA are α1 and α2 and their physiological role is controlled both by their unique and independent signalling pathways, and their discrete subcellular distribution.

70 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Na+/K+ ATPase Inhibitors & Modulators

(+)-SJ733 Acevaltrate (SJ000557733) Cat. No.: HY-19556 Cat. No.: HY-N2070

Bioactivity: (+)-SJ733 is a clinical candidate for malaria which can Bioactivity: Acevaltrate, isolated from Valeriana glechomifolia, inhibits also inhibit Na+-ATPase PfATP4. the Na+/ K+-ATPase activity in the rat kidney and brain

hemispheres with IC50s of 22.8±1.1 μM and 42.3±1.0 μM, respectively [1]. Purity: 99.45% Purity: 99.56% Clinical Data: Phase 1 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, 25 mg, 50 mg, 100 mg

Bufalin Cat. No.: HY-N0877 Cat. No.: HY-B1429

Bioactivity: Bufalin is an active component isolated from Chan Su, acts as Bioactivity: Chlorpropamide is an oral antihyperglycemic agent used for the a potent Na+/K+-ATPase inhibitor, binds to the subunit α1, treatment of non-insulin-dependent diabetes mellitus (NIDDM). [1] α2 and α3, with Kd of 42.5, 45 and 40 nM, respectively [2]. Anti-cancer activity [2]. Purity: 98.85% Purity: 99.24% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 100 mg

Digitoxin Cat. No.: HY-B1357 (12β-Hydroxydigitoxin) Cat. No.: HY-B1049

Bioactivity: is an effective Na+/K+-ATPase inhibitor, the EC50 Bioactivity: Digoxin is a potent inhibitor of Na+/K+-ATPase, clinically value of Digitoxin is 0.78 μM. used to treat and .

Purity: 99.18% Purity: 98.92% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg 100 mg, 500 mg

Ginsenoside Rb1 Istaroxime (Gypenoside III) Cat. No.: HY-N0039 (PST2744) Cat. No.: HY-15718

Bioactivity: Ginsenoside Rb1, a main constituent of the root of Panax Bioactivity: Istaroxime (PST2744) is a potent inhibitor of Na+,K+-ATPase ginseng, inhibits Na+, K+-ATPase activity with an IC of 50 with IC50 of 0.11 μM. 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65 . Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg

Istaroxime hydrochloride Oleandrin (PST2744 (hydrochloride)) Cat. No.: HY-15718A Cat. No.: HY-13719

Bioactivity: Istaroxime hydrochloride is a Na+/K+-ATPase inhibitor ( Bioactivity: Oleandrin inhibits the Na+, K+-ATPase activity with an

IC50=0.11 μM) and a sarcoplasmic/endoplasmic reticulum calcium IC50 of 620 nM. ATPase 2 ( SERCA 2) activator.

Purity: 99.32% Purity: 99.84% 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 2 mg, 5 mg, 10 mg, 25 mg

www.MedChemExpress.com 71

Ouabain Octahydrate Phlorizin (Acocantherine; G-Strophanthin) Cat. No.: HY-B0542 (Floridzin; NSC 2833) Cat. No.: HY-N0143

+ + Bioactivity: Octahydrate is an inhibitor of Na /K -ATPase, used Bioactivity: Phlorizin is a non-selective SGLT inhibitor with Kis of 300 for the treatment of congestive heart failure. and 39 nM for hSGLT1 and hSGLT2, respectively. Phlorizin is also a Na+/K+-ATPase inhibitor.

Purity: 99.91% Purity: 95.33% 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

Prilocaine hydrochloride Cat. No.: HY-B0137 Cat. No.: HY-B0137A

Bioactivity: Prilocaine is a local anesthetic of the amino amide type. Bioactivity: Prilocaine hydrochloride is a local anesthetic of the amino amide type.

Purity: 96.81% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg, 500 mg 50 mg, 100 mg

Rostafuroxin (PST 2238) Cat. No.: HY-12283

Bioactivity: Rostafuroxin(PST 2238) is a antihypertensive compound; Na,K-ATPase antognist;displaced [3H]ouabain from the dogkidney Na+,K+-ATPase with IC50 of 1.5 nM.

Purity: 96.70% Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

72 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] nAChR Nicotinic acetylcholine receptors

nAChRs (nicotinic acetylcholine receptors) are neuron 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 —hence the name "nicotinic".

www.MedChemExpress.com 73 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 (; 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

74 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 Decamethonium 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 Dinotefuran (Deformylflustrabromine hydrochloride; dFBr hydrochloride) Cat. No.: HY-107675 (MTI-446) Cat. No.: HY-B0827

Bioactivity: Desformylflustrabromine hydrochloride is a selective agonist Bioactivity: Dinotefuran is an insecticide of the neonicotinoid class, its

of α4β2 neuronal nicotinic acetylcholine receptor ( nAChR) mechanism of action 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 75

GTS-21 dihydrochloride Hexamethonium 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: Methyllycaconitine 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 nicotinic antagonist. 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

76 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 77

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 smoking 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: Vecuronium bromide 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 estrogen-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

78 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] NKCC Na-K-Cl cotransporter;Na(+)-K(+)-Cl(-) cotransporter;Na+-K+-Cl− cotransporter

NKCC (Na-K-Cl cotransporter) is a protein that aids in the active transport of sodium, potassium, and chloride into and out of cells. There are two varieties of this membrane transport protein, NKCC1 and NKCC2, however these are encoded by two different genes (SLC12A2 and SLC12A1 respectively) and are not isoforms. Two isoforms of the NKCC1/Slc12a2 gene result from keeping (isoform 1) or skipping (isoform 2) exon 21 in the final gene product. NKCC1 is widely distributed throughout the body; it has important functions in organs that secrete fluids. NKCC2 is found specifically in the kidney, where it serves to extract sodium, potassium, and chloride from the urine so that they can be reabsorbed into the blood. NKCC proteins are membrane transport proteins that transport sodium (Na), potassium (K), and chloride (Cl) ions across the cell membrane. Because they move each solute in the same direction, NKCC proteins are considered symporters.

www.MedChemExpress.com 79 NKCC Inhibitors & Modulators

Bumetanide (Ro 10-6338; PF 1593) Cat. No.: HY-17468 Cat. No.: HY-B0135

Bioactivity: (Ro 10-6338; PF 1593) is an inhibitor of Bioactivity: Furosemide (Lasix) is a inhibitor of Na+/2Cl-/K+ Na(+)-K(+)-2Cl(-) co-transporter (NKCC) with an IC50 of 0.6 (NKCC) cotransporter of which used in the treatment of uM. congestive heart failure and edema.

Purity: 99.91% Purity: 99.83% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 1 g, 5 g

Furosemide sodium Cat. No.: HY-B0135A

Bioactivity: Furosemide sodium (Lasix) is a loop diuretic inhibitor of Na+/2Cl-/K+ (NKCC) cotransporter of which used in the treatment of congestive heart failure and edema.

Purity: 99.69% Clinical Data: Launched Size: 10mM x 1mL in DMSO, 1 g

80 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] P-glycoprotein P-gp;Pgp;Multidrug resistance protein 1;MDR1;ATP-binding cassette sub-family B member 1;ABCB1;Cluster of differentiation 243;CD243

P-glycoprotein (P-gp) also known as multidrug resistance protein 1 (MDR1) is an important protein of the cell membrane that pumps many foreign substances out of cells. More formally, it is an ATP-dependent efflux pump with broad substrate specificity. P-gp is extensively distributed and expressed in the intestinal epithelium where it pumps xenobiotics (such as toxins or drugs) back into the intestinal lumen, in liver cells where it pumps them into bile ducts, in the cells of the proximal tubular of the kidney where it pumps them into urine-conducting ducts, and in the capillary endothelial cells comprising the blood–brain barrier and blood-testis barrier, where it pumps them back into the capillaries. Some cancer cells also express large amounts of P-gp, which renders these cancers multi-drug resistant. P-gp is an ATP-dependent drug efflux pump for xenobiotic compounds with broad substrate specificity. It is responsible for decreased drug accumulation in multidrug-resistant cells and often mediates the development of resistance to anticancer drugs. This protein also functions as a transporter in the blood–brain barrier.

www.MedChemExpress.com 81 P-glycoprotein Inhibitors & Modulators

(20S)-Protopanaxadiol Alisol F (20-Epiprotopanaxadiol; 20(S)-APPD) Cat. No.: HY-N0797 Cat. No.: HY-N0854

Bioactivity: (20S)-Protopanaxadiol (20-Epiprotopanaxadiol) is an aglycon Bioactivity: Alisol F is a natural product. metabolic derivative of the protopanaxadiol-type ginseng saponin; apoptosis inducer. IC50 value: Target: apoptosis inducer (20S)-Protopanaxadiol was used to induce cytotoxicity for two human glioma cell lines, SF188 and U87MG. For the… Purity: 98.0% Purity: 96.20% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg 10 mg, 50 mg

Biricodar Dofequidar (VX-710) Cat. No.: HY-13574A Cat. No.: HY-17013

Bioactivity: Biricodar (VX-710) is a modulator of P-glycoprotein and Bioactivity: Dofequidar(MS-209) is a novel compound, which can MRP-1; shows effective chemosensitizing activity in reverse P-glycoprotein (P-gp)-mediated MDR. multidrug resistant cells.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 5 mg, 10 mg, 50 mg, 100 mg

Dofequidar fumarate Elacridar (MS-209) Cat. No.: HY-17013A (GF120918; GW0918; GG918; GW120918) Cat. No.: HY-50879

Bioactivity: Dofequidar fumarate(MS-209 fumarate), an orally active Bioactivity: Elacridar is a potent P-glycoprotein (Pgp) and BCRP quinoline compound, has been reported to overcome MDR by inhibitor. inhibiting ABCB1/P-gp, ABCC1/MDR-associated protein 1, or both.

Purity: 99.99% Purity: 98.47% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg, 100 mg, 200 mg, 500 mg 5 mg, 10 mg, 50 mg, 100 mg

Elacridar hydrochloride Encequidar (GF120918A) Cat. No.: HY-50880 (HM30181; HM30181A) Cat. No.: HY-13646

Bioactivity: Elacridar Hcl (GF120918; GW0918) is a P-glycoprotein Bioactivity: Encequidar (HM30181) is a potent and selective inhibitor of inhibitor, and has been used both in vitro and in vivo as a P-glycoprotein. tool inhibitor of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules. IC50 value: Target: P-glycoprotein In vitro, GF120918A… Purity: 98.87% Purity: 98.12% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Encequidar mesylate MCI826 (HM30181 (mesylate); HM30181A (mesylate)) Cat. No.: HY-13646A Cat. No.: HY-U00247

Bioactivity: Encequidar (mesylate) (HM30181 (mesylate)) is a competitive Bioactivity: MCI826 is a P-glycoprotein ( P-gp) antagonist. and potent P-glycoprotein inhibitor.

Purity: 99.76% 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

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

NSC23925 P-gp inhibitor 1 Cat. No.: HY-19626 Cat. No.: HY-101791

Bioactivity: NSC23925 is a novel, selective and effective P-glycoprotein ( Bioactivity: P-gp inhibitor 1 is a novel inhibitor reversing Pgp) inhibitor. P-glycoprotein-mediated multidrug resistance.

Purity: 99.23% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 100 mg, 250 mg, 500 mg 5 mg, 10 mg, 25 mg

P-gp modulator 1 Cat. No.: HY-112912 (Bioperine; 1-Piperoylpiperidine) Cat. No.: HY-N0144

Bioactivity: P-gp modulator 1 is a high affinity, orally available Bioactivity: Piperine, a natural alkaloid isolated from Piper nigrum L,

modulator of P-glycoprotein (Pgp), can reverse the inhibits P-glycoprotein and CYP3A4 activities with an IC50 [1] Pgp-mediated multidrug resistance ((MDR) . value of 61.94±0.054 μg/mL in HeLa cell.

Purity: >98% Purity: 98.76% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 100 mg, 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 200 mg, 1 g, 5 g

Polyoxyethylene stearate Reversan (POES) Cat. No.: HY-101530 (CBLC4H10) Cat. No.: HY-107643

Bioactivity: Polyoxyethylene stearate (POES) is a non-ionic emulsifying Bioactivity: Reversan (CBLC4H10) is a potent and nontoxic multidrug agent. resistance-associated protein 1 (MRP1) and P-glycoprotein (Pgp) inhibitor [1] [2].

Purity: Purity: 95.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 2 mg, 5 mg 200 mg, 1 g, 5 g

Risperidone Sinapine (R 64 766) Cat. No.: HY-11018 Cat. No.: HY-N5077

Bioactivity: is a serotonin 5-HT2 receptor blocker, Bioactivity: Sinapine is an alkaloid from seeds of the cruciferous species P-Glycoprotein inhibitor and potent dopamine D receptor which shows favorable biological activities such as 2 antioxidant and radio-protective activities. antagonist, with Kis of 4.8, 5.9 nM for 5-HT 2A and dopamine

D 2 receptor, respectively. Purity: 99.16% Purity: 99.72% 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

Sinapine thiocyanate Tariquidar Cat. No.: HY-N0450 (XR9576) Cat. No.: HY-10550

Bioactivity: Sinapine is an alkaloid from seeds of the cruciferous species Bioactivity: Tariquidar is a potent and specific inhibitor of P-glycoprotein

which shows favorable biological activities such as ( P-gp) with the high affinity ( Kd=5.1±0.9 nM). antioxidant and radio-protective activities.

Purity: 98.32% Purity: 98.57% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 83

Tariquidar methanesulfonate, hydrate Valspodar (XR9576 (methanesulfonate, hydrate)) Cat. No.: HY-10550A (PSC 833) Cat. No.: HY-17384

Bioactivity: Tariquidar methanesulfonate, hydrate is a potent and specific Bioactivity: Valspodar is a selective P-glycoprotein inhibitor that has been

inhibitor of P-glycoprotein ( P-gp) with a Kd of 5.1 nM. used as an experimental cancer treatment and chemosensitizer.

Purity: 98.02% Purity: 99.27% Clinical Data: Phase 3 Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 5 mg, 10 mg

Zamicastat Zosuquidar (BIA 5-1058) Cat. No.: HY-106004 (LY335979) Cat. No.: HY-15255

Bioactivity: Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) Bioactivity: Zosuquidar (LY335979) is a potent negative modulator of inhibitor that could cross the blood-brain barrier (BBB) and P-glycoprotein-mediated multi-drug resistance with Ki of 60 cause central as well as peripheral effects. Zamicastat is nM. IC50 value: 60 nM (Ki) Target: P-glycoprotein Zosuquidar also a concentration-dependent dual P-gp and BCRP inhibitor (LY335979) is a potent modulator of P-glycoprotein-mediated [1] multidrug resistance with Ki of 60 nM. Zosuquidar binds with… with IC50 values of 73.8 μM and 17.0 μM, respectively .… Purity: 99.95% Purity: 98.33% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Zosuquidar trihydrochloride (RS 33295-198 trihydrochloride; LY-335979 trihydrochloride) Cat. No.: HY-50671

Bioactivity: Zosuquidar trihydrochloride is an inhibitor of P-glycoprotein

with a Ki value of 59 nM.

Purity: 98.75% Clinical Data: Phase 3 Size: 10 mg, 50 mg, 100 mg

84 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] P2X Receptor P2XRs

P2X receptors are a family of cation-permeable ligand gated ion channels that open in response to the binding of extracellular 5'-triphosphate (ATP). They belong to a larger family of receptors known as the purinergic receptors. P2X receptors are present in a diverse array of organisms including humans, mouse, rat, rabbit, chicken, zebrafish, bullfrog, fluke, and amoeba. seven separate genes coding for P2X subunits have been identified, and named to as P2X1 through P2X7. The pharmacology of a given P2X receptor is largely determined by its subunit makeup. Different subunits exhibit different sensitivities to purinergic agonists and antagonists. Of continuing interest is the fact that some P2X receptors (P2X2, P2X4, human P2X5, and P2X7) exhibit multiple open states in response to ATP, characterized by a time-dependent increase in the permeabilities of large organic ions and nucleotide binding dyes.

www.MedChemExpress.com 85 P2X Receptor Inhibitors & Modulators

A 438079 A 438079 (hydrochloride) Cat. No.: HY-15488 Cat. No.: HY-15488A

Bioactivity: A 438079 is a potent, and selective P2X7 Bioactivity: A 438079 (hydrochloride) is a potent, and selective P2X receptor antagonist with pIC 50 of 6.9. receptor antagonist with pIC 50 of 6.9. 7

Purity: 99.64% Purity: 99.88% 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

A 839977 A-317491 Cat. No.: HY-13954 Cat. No.: HY-15568

Bioactivity: A-839977 is a novel and selective P2X7 antagonist; blocks Bioactivity: A-317491 is a non-nucleotide P2X3 and P2X2/3 receptor BzATP-evoked calcium influx at recombinant human, rat and antagonist, which inhibits calcium flux mediated by the mouse P2X7 receptors (IC50 values are 20, 42 and 150 nM receptors. IC50 value: Target: P2X2/3 It is known that P2X3 respectively). and P2X2/3 receptors stimulate the pronociceptive effects of ATP upon activation. Studies indicate that the P2X3 receptor… Purity: 98.74% Purity: 99.18% 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, 50 mg

A-317491 sodium salt hydrate A-740003 Cat. No.: HY-15568A Cat. No.: HY-50697

Bioactivity: A-317491 is a non-nucleotide P2X3 and P2X2/3 receptor Bioactivity: A-740003 is a potent, selective and competitive P2X7 antagonist, which inhibits calcium flux mediated by the receptor antagonist with IC50 values are 18 and 40 nM for rat receptors. IC50 value: Target: P2X2/3 receptor It is known and human P2X7 receptors, respectively. that P2X3 and P2X2/3 receptors stimulate the pronociceptive effects of ATP upon activation. Studies indicate that the P2X3… Purity: 99.65% Purity: 98.91% 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 10 mg, 50 mg, 100 mg

A-804598 AF-353 Cat. No.: HY-100483 (Ro-4) Cat. No.: HY-14483

Bioactivity: A-804598 is a novel, competitive, and selective P2X7 receptor Bioactivity: AF-353 is a novel, potent and orally bioavailable P2X3/P2X2/3 antagonist with IC50 of 10 nM, 9 nM and 11 nM in rat, mouse receptor antagonist, inhibits human and rat P2X3 (pIC50= 8.0). and human P2X7 receptors respectively. In vitro: A-804598 potently blocked IL-1β release in the THP-1 cells (IC50 of 8.5 nM). A-804598 also blocked agonist-evoked pore formation in… Purity: 98.83% Purity: 98.95% 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

ATP disodium salt (Disodium adenosine triphosphate; Adenosine AZD9056 hydrochloride 5'-triphosphate disodium salt) Cat. No.: HY-B0345A Cat. No.: HY-19427A

Bioactivity: ATP is a phosphate-group donor for substrate activation in Bioactivity: AZD9056 is a selective orally active inhibitor of P2X7 which metabolic reactions and the coenzyme for a large number of plays a significant role in inflammation and pain-causing kinases. diseases.

Purity: 98.0% Purity: 98.10% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 1 g, 5 g 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

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

CE-224535 Gefapixant (PF-04905428) Cat. No.: HY-15487 (AF219; MK-7264) Cat. No.: HY-101588

Bioactivity: CE-224535 is a selective P2X7 receptor antagonist. Bioactivity: Gefapixant is an orally active P2X3 receptor ( P2X3R) antagonist with IC 50s of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.

Purity: >98% Purity: 99.62% Clinical Data: Phase 2 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

GW791343 dihydrochloride GW791343 trihydrochloride Cat. No.: HY-15469 Cat. No.: HY-15470

Bioactivity: GW791343 2Hcl is a P2X7 allosteric modulator; exhibits Bioactivity: GW791343 3Hcl is a P2X7 allosteric modulator; exhibits species-specific activity and acts as a negative allosteric species-specific activity and acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2). modulator of human P2X7 (pIC50 = 6.9 - 7.2).

Purity: 94.07% 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, 50 mg

JNJ-54175446 KN-62 Cat. No.: HY-117508 Cat. No.: HY-13290

Bioactivity: JNJ-54175446 is a potent and selective brain penetrant P2X7 Bioactivity: KN-62 is a selective and potent inhibitor of calmodulin-dependent protein kinase II ( CaMK-II) with IC receptor antagonist, with pIC50s of 8.46 and 8.81 for hP2X7 50 receptor and rP2X7 receptor, respectively. of 0.9 μM, KN-62 also displays noncompetitive antagonism at

P2X7 receptors in HEK293 cells, with an IC50 value… Purity: >98% Purity: 99.16% 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

Lappaconitine PSB-12062 ((+)-Lappaconitine) Cat. No.: HY-N0383 (N-(p-Methylphenylsulfonyl)phenoxazine) Cat. No.: HY-101910

Bioactivity: Lappaconitine, isolated from Aconitum sinomontanum Nakai, was Bioactivity: PSB-12062 is a potent and selective P2X4 antagonist with an characterized as analgesic principle. IC50 of 1.38 μM for human P2X4.

Purity: >98% Purity: 98.45% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

www.MedChemExpress.com 87 Potassium Channel KcsA

Potassium channels are the most widely distributed type of ion channel and are found in virtually all living organisms. They form potassium-selective pores that span cell membranes. Potassium channels are found in most cell types and control a wide variety of cell functions. Potassium channels function to conduct potassium ions down their electrochemical gradient, doing so both rapidly and selectively. Biologically, these channels act to set or reset the resting potential in many cells. In excitable cells, such asneurons, the delayed counterflow of potassium ions shapes the . By contributing to the regulation of the action potential duration in cardiac muscle, malfunction of potassium channels may cause life-threatening . Potassium channels may also be involved in maintaining vascular tone.

88 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Potassium Channel Inhibitors & Modulators

20-HETE 4-Aminopyridine (20-hydroxy ) Cat. No.: HY-15598 (4-AP; 4-Pyridinamine; Fampridine) Cat. No.: HY-B0604

Bioactivity: 20-HETE(20-hydroxy Arachidonic Acid) is a potent Bioactivity: 4-Aminopyridine is a nonselective K+ channel blocker that vasoconstrictor produced in vascular smooth muscle (VSM) binds from the cytoplasmic side of the cell membrane. cells. It depolarizes VSM by blocking the open-state probability of Ca2+-activated K+-channels. IC50 Value: Target: 20-Hydroxyeicosatetraenoic acid (20-HETE) is a cytochrome… Purity: 95.0% Purity: 99.97% Clinical Data: No Development Reported Clinical Data: Launched Size: 2 mg, 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 g, 10 g

Acacetin (5,7-Dihydroxy-4'-methoxyflavone) Cat. No.: HY-N0451 (Cardiorythmine; (+)-Ajmaline) Cat. No.: HY-B1167

Bioactivity: 1) Natural acacetin was a 4.0-fold and 5.5-fold more potent Bioactivity: Ajmaline is an alkaloid that is class Ia antiarrhythmic agent. inhibitor of BACE-1 than oleanolic acid and maslinic acid, respectively.[1] 2) Acacetin significantly suppressed the photoreceptor collapse. [1] 3) Acacetin significantly reduces the Aβ levels by interfering with human APP proteolytic… Purity: 98.43% Purity: 99.31% 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

Almitrine mesylate ( bismesylate; Almitrine bismethanesulfonate; Almitrine dimesylate) Cat. No.: HY-107319 (H 234​/09) Cat. No.: HY-106855

Bioactivity: Almitrine mesylate, a peripheral chemoreceptor agonist, Bioactivity: Almokalant is a class III antiarrhythmic drug, acts as a inhibits selectively the Ca 2+-dependent K+ channel. potassium channel blocker, and inhibits a specific component (Ikr) of the time-dependent delayed rectifier K + current.

Purity: 99.36% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 10 mg, 50 mg, 100 mg

Amiodarone hydrochloride Cat. No.: HY-14187 Cat. No.: HY-14188

Bioactivity: Amiodarone is an antiarrhythmic drug for inhibition of Bioactivity: Amiodarone is an antiarrhythmic drug for inhibition of

ATP-sensitive potassium channel with an IC 50 of 19.1 μM. ATP-sensitive potassium channel with IC50 of 19.1 μM. IC50 Value: 1.5 uM ( inhibit TBARS, LOOH and FPL formation)[1] in vitro: It was found that 10 uM amiodarone induces accumulation of ethidium bromide (5 ug/ml) in Saccharomyces cerevisiae… Purity: >98% Purity: 99.82% Clinical Data: Launched Clinical Data: Launched Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 1 g, 5 g

Antihistamine-1 Apamin (Apamin (reduced), cyclic Cat. No.: HY-100238 (1→11),(3→15)-bis(disulfide); Apamine) Cat. No.: HY-P0256

Bioactivity: Antihistamine-1 is a H1-antihistamine ( Ki=6.9 nM) with Bioactivity: Apamin, an 18 amino acid peptide found in apitoxin 2+ + acceptable blood-brain barrier penetration and also an (bee venom), is known to block Ca -activated K channels and prevent carbon tetrachloride-induced liver fibrosis. inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 500u g, 1 mg

www.MedChemExpress.com 89

Astemizole AUT1 (R 43512) Cat. No.: HY-12532 Cat. No.: HY-117639

Bioactivity: , a second-generation antihistamine drug to diminish Bioactivity: AUT1 is a Kv3 potassium channel modulator, with pEC50s of allergic symptoms with a long duration of action, is a 5.33 and 5.31 for human recombinant Kv3.1b and Kv3.2a, histamine H1-receptor antagonist, with an IC of 4 nM. 50 respectively, exhibits 10-fold lower potency at human Astemizole also shows potent hERG K+ channel blocking activ… [1] recombinant Kv3.3 channel ( pEC50, 4.5) . Purity: >98% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Azimilide Dihydrochloride (NE-10064) Cat. No.: HY-18600 (NE-10064 Dihydrochloride) Cat. No.: HY-18600A

Bioactivity: Azimilide(NE-10064) is a class III antiarrhythmic compound, Bioactivity: Azimilide 2Hcl(NE-10064 2Hcl) is a class III antiarrhythmic inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac I(Ks) (minK) channels expressed in Xenopus oocytes. myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes. IC50 value: Target: in vitro: Azimilide blocked HERG channels at 0.1 and 1 Hz with IC50s of 1.4 microM and 5.2… Purity: >98% Purity: 98.35% 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

BMS-191011 BMS-191095 (BMS-A) Cat. No.: HY-108593 Cat. No.: HY-14256

Bioactivity: BMS-191011 (BMS-A) is an opener of the large-conductance, Bioactivity: BMS-191095 is an activators of mitochondrial ATP-sensitive Ca2++-activated potassium (maxi-K) channel, effective in stroke potassium (mitoKATP) channels. models [1].

Purity: >98% Purity: 98.06% 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, 5 mg, 10 mg, 25 mg, 50 mg

Butamben D6 hydrochloride (Butyl 4-aminobenzoate) Cat. No.: HY-B1430 Cat. No.: HY-B0407AS

Bioactivity: is a long-duration local anesthetic used for the Bioactivity: Chlorpromazine D6 hydrochloride is the deuterium labeled treatment of chronic pain. Chlorpromazine. Chlorpromazine is an inhibitor of dopamine receptor, 5-HT receptor, potassium channel, sodium channel.

Purity: 98.0% Purity: 99.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 g 1 mg, 5 mg, 10 mg

Chlorpromazine hydrochloride Cholesterol myristate Cat. No.: HY-B0407A (Cholesteryl myristate; Cholesteryl tetradecanoate) Cat. No.: HY-N2338

Bioactivity: Chlorpromazine Hydrochloride is an antagonist of the Bioactivity: Cholesterol myristate is a natural steroid present in dopamine D2, 5HT2A, potassium channel and sodium traditional Chinese medicine. Cholesterol myristate binds to

channel. Chlorpromazine binds with D2 and 5HT2A with Kis of 363 several ion channels such as the nicotinic acetylcholine nM and 8.3 nM, respectively. receptor, GABAA receptor, and the inward-rectifier potassium ion channel. Purity: 99.83% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 1 g, 5 g Size: 250 mg

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

Clofilium tosylate fendizoate Cat. No.: HY-33350 Cat. No.: HY-B2179

Bioactivity: Clofilium tosylate, a potassium channel blocker, induces Bioactivity: Cloperastine fendizoate inhibits the hERG K+ currents in a apoptosis of human promyelocytic leukemia (HL-60) cells via concentration-dependent manner with an IC50 value of 27 nM. Bcl-2-insensitive activation of caspase-3. Antiarrhythmic agent [1].

Purity: 99.77% Purity: 99.38% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 100 mg

Daurisoline DCEBIO ((R,R)-Daurisoline) Cat. No.: HY-N0221 Cat. No.: HY-102052

Bioactivity: Daurisoline is a hERG inhibitor and also an autophagy Bioactivity: DCEBIO, a derivative of 1-EBIO, is an extremely potent blocker. activator of Cl secretion in T84 colonic cells [1]. DCEBIO stimulates Cl secretion via the activation of hIK1 K channels and the activation of an apical membrane Cl Purity: 98.02% 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

DCPIB Dequalinium Chloride Cat. No.: HY-103371 Cat. No.: HY-B0567

Bioactivity: DCPIB is a selective, reversible and potent inhibitor of Bioactivity: Dequalinium Chloride is a selective blocker of volume-regulated anion channels ( VRAC), voltage-dependently apamin-sensitive K+ channels. activates potassium channels TREK1 and TRAAK, inhibits TRESK,

TASK1 and TASK3 ( IC50s, 0.14, 0.95, 50.72 μM, respective…

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

Diazoxide DMP-543 (Sch-6783; SRG-95213) Cat. No.: HY-B1140 (XR-543) Cat. No.: HY-108590

Bioactivity: is an ATP-sensitive potassium channel activator ; Bioactivity: DMP-543 (XR-543) is a KV7 channel blocker, also acts as a can be used to treat hyperinsulinism. potent neurotransmitter release enhancer [1] [2].

Purity: 99.99% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 100 mg

Dofetilide Domiphen bromide (UK 68789) Cat. No.: HY-B0232 Cat. No.: HY-B1467

Bioactivity: (Tikosyn) is a class III antiarrhythmic agent. Bioactivity: Domiphen bromide is a chemical antiseptic and a quaternary ammonium compound, used as a cationic surfactant.

Purity: 98.77% Purity: 98.0% 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 g

www.MedChemExpress.com 91

Doxapram hydrochloride hydrate Cat. No.: HY-B0551 Cat. No.: HY-B0551A

Bioactivity: Doxapram inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric Bioactivity: Doxapram hydrochloride hydrate inhibits TASK-1, TASK-3, channel function with EC50 of 410 nM, 37 μM, 9 μM, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 respectively. nM, 37 μM, 9 μM, respectively.

Purity: >98% Purity: 98.86% Clinical Data: Launched Clinical Data: Launched Size: 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 50 mg, 100 mg

Dronedarone Hydrochloride E-4031 Cat. No.: HY-75839 Cat. No.: HY-15551

Bioactivity: hydrochloride is a non-iodinated amiodarone Bioactivity: E-4031 is a class III antiarrhythmic agent which derivative that inhibits Na+, K+ and Ca2+ currents. selectively blocks hERG potassium channel.

Purity: 99.93% Purity: 98.03% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 10 mg, 50 mg 5 mg, 10 mg, 50 mg

Endoxifen Z-isomer Endoxifen Z-isomer hydrochloride Cat. No.: HY-18719 Cat. No.: HY-18719A

Bioactivity: Endoxifen Z-isomer is the most important metabolite Bioactivity: Endoxifen Z-isomer hydrochloride is the most important responsible for eliciting the anti-estrogenic effects of this Tamoxifen metabolite responsible for eliciting the drug in breast cancer cells expressing estrogen receptor-alpha anti-estrogenic effects of this drug in breast cancer cells (ERα). Endoxifen inhibits hERG tail currents at 50 mV in a expressing estrogen receptor-alpha (ERα). Endoxifen inhibits concentration-dependent manner with IC50 values of 1.6 μM.… hERG tail currents at 50 mV in a concentration-dependent… Purity: >98% Purity: 99.31% 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 1 mg, 5 mg, 10 mg

Eucalyptol Flufenamic acid (1,8-Cineole) Cat. No.: HY-N0066 Cat. No.: HY-B1221

Bioactivity: is an inhibitor of 5-HT3 receptor , potassium Bioactivity: Flufenamic acid is a non-steroidal anti-inflammatory agent, channel, TNF-α and IL-1β. inhibits cyclooxygenase ( COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selective cation channel…

Purity: 98.0% Purity: 99.92% Clinical Data: Phase 3 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg 100 mg

Flupirtine 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. channel opener 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

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

GAL-021 Ginsenoside Rg3 Cat. No.: HY-101422 (20(S)-Ginsenoside-Rg3; Rg3; S-Ginsenoside Rg3) Cat. No.: HY-N0603

Bioactivity: GAL-021 a new intravenous BKCa-channel blocker. Bioactivity: Ginsenoside Rg3 is the main component of Red ginseng. Ginsenoside Rg3 inhibits Na+ and hKv1.4 channel with IC

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: 98.0% 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, 100 mg 10 mg, 50 mg, 100 mg

Glibenclamide (Glyburide) Cat. No.: HY-15206 (S1702; SE1702) Cat. No.: HY-B0753

Bioactivity: is a selective inhibitor of ATP-sensitive K+ Bioactivity: Gliclazide is a whole-cell beta-cell ATP-sensitive potassium channel. currents blocker with an IC50 of 184 nM.

Purity: 98.0% Purity: 96.99% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 1 g, 5 g

Glipizide GSK369796 Dihydrochloride (CP 28720; K 4024) Cat. No.: HY-B0254 Cat. No.: HY-12082A

Bioactivity: is used to treat high blood sugar levels caused by a Bioactivity: GSK369796 Dihydrochloride is an affordable and effective type of diabetes mellitus called type 2 diabetes. antimalarial and inhibits hERG potassium ion channel

repolarization with an IC50 of 7.5 μM.

Purity: 99.47% Purity: 99.94% Clinical Data: Launched Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

Hexachlorophene HMR 1556 (Hexachlorofen) Cat. No.: HY-12637 Cat. No.: HY-106369

Bioactivity: Hexachlorophene (Hexachlorofen) is a highly effective Bioactivity: HMR 1556, a chromanol derivative, is a IKs blocker with IC50s antibacterial agent, causes lysis of protoplasts and leakage of of 10.5 nM and 34 nM in canine and guinea pig left ventricular intracellular contents in bacterial at high concentrations myocytes, respectively [1] [2]. [1]. Hexachlorophene (Hexachlorofen) is also a KCNQ1/KCNE1<…

Purity: 99.66% Purity: 99.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg 1 g, 5 g

ICA 110381 ICA-069673 Cat. No.: HY-108587 Cat. No.: HY-101396

Bioactivity: ICA 110381 (Compound 16) is a KCNQ2/Q3 potassium channel Bioactivity: ICA-069673 is a KCNQ2/Q3 potassium channel activator with an

opener for the treatment of epilepsy. ICA 110381 is a KCNQ2/ IC50 of 0.69 μM. Q3 agonist ( EC50=0.38 μM) as well as KCNQ1 antagonist ( [1] IC50=15 μM) . Purity: >98% Purity: 98.12% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

www.MedChemExpress.com 93

Indapamide Ketanserin Cat. No.: HY-B0259 (R41468) Cat. No.: HY-10562

Bioactivity: is a non- sulphonamide diuretic compound, Bioactivity: Ketanserin is a selective 5-HT receptor antagonist. generally used in the treatment of hypertension, as well as Ketanserin also blocks hERG current ( IhERG) in a decompensated cardiac failure. concentration-dependent manner ( IC50=0.11 μM).

Purity: 99.61% Purity: 98.86% 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

Ketanserin tartrate KRN4884 (R41468 tartrate) Cat. No.: HY-10562A Cat. No.: HY-U00201

Bioactivity: Ketanserin tartrate is a selective 5-HT receptor antagonist. Bioactivity: KRN4884 is a K+ channel opener. In the presence of Ketanserin tartrate also blocks hERG current ( I ) in a hERG intracellular ATP (1 mM), KRN4884 (0.1-3 μM) activates KATP concentration-dependent manner ( IC =0.11 μM). 50 channels in a concentration-dependent manner ( EC50=0.55 μM). Purity: 99.97% 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 50 mg, 100 mg

Kv3 modulator 1 Levcromakalim Cat. No.: HY-111996 ((-)-; BRL 38227) Cat. No.: HY-14255

Bioactivity: Kv3 modulator 1 is a Kv3 voltage-gated potassium channel Bioactivity: + LevCromakalim is an ATP-sensitive K channel (K ATP) modulator extracted from patent WO2018020263A1, Compound X. activator. Kv3 modulator 1 can be used to treat inflammatory pain [1].

Purity: >98% Purity: 99.76% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

Loureirin B LY 303511 Cat. No.: HY-N1504 Cat. No.: HY-15643

Bioactivity: Loureirin B, a extracted from Dracaena Bioactivity: LY303511 is a structural analogue of LY294002. LY303511 does cochinchinensis, is an inhibitor of plasminogen activator not inhibit PI3K. LY303511 enhances TRAIL sensitivity of SHEP-1 + inhibitor-1 (PAI-1), with an IC 50 of 26.10μM; Loureirin B neuroblastoma cells. LY303511 reversibly blocks K currents (IC =64.6±9.1 μM) in MIN6 insulinoma cells. also inhibits KATP, the phosphorylation of ERK and JNK 50 Purity: 99.99% 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

LY 303511 hydrochloride MCHr1 antagonist 2 Cat. No.: HY-15643A Cat. No.: HY-100321

Bioactivity: LY 303511 hydrochloride is a structural analogue of LY294002. Bioactivity: MCHr1 antagonist 2 is an antagonist of melanin

LY303511 does not inhibit PI3K. LY303511 enhances TRAIL concentrating hormone receptor 1, with an IC50 of 65 nM; sensitivity of SHEP-1 neuroblastoma cells. LY303511 reversibly MCHr1 antagonist 2 also inhibits hERG, with an IC50 of 4.0 nM blocks K+ currents (IC =64.6±9.1 μM) in MIN6 insulinoma 50 in IMR-32 cells. cells. Purity: 98.41% 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

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

Minoxidil Calcium (U10858) Cat. No.: HY-B0112 (KAD-1229; S21403) Cat. No.: HY-17398

Bioactivity: (U 10858) is an antihypertensive vasodilator Bioactivity: Mitiglinide(KAD-1229; S21403) is a drug for the treatment of medication. Target: potassium channel Minoxidil, a potent type 2 diabetes; it is a highly selective KATP channel antihypertensive agent, induces generalized hypertrichosis antagonist. when administered systemically, or localized hair regrowth when applied topically to sites of severe alopecia areata. The… Purity: 99.96% Purity: 98.88% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 100 mg, 200 mg, 500 mg

Mitiglinide calcium hydrate MK-7145 (KAD-1229 calcium hydrate; S-21403 calcium hydrate) Cat. No.: HY-B0682A Cat. No.: HY-18277

Bioactivity: Mitiglinide calcium hydrate is a drug for the treatment of Bioactivity: MK-7145 is a ROMK inhibitor, with an IC50 of 0.045 μM. type 2 diabetes; it is a highly selective KATP channel antagonist.

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

ML133 hydrochloride ML213 Cat. No.: HY-100230A Cat. No.: HY-101843

Bioactivity: ML133 (hydrochloride) is a selective Kir2 family channels Bioactivity: ML213 is a selective activator of Kv7.2 and Kv7.4 channels, enhances Kv7.2 and Kv7.4 channels with EC50s of 230 and 510 inhibitor, with an IC50 of 1.8 μM at pH 7.4 and 290 nM at pH nM, respectively. 8.5 [1].

Purity: >98% Purity: 99.53% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

ML277 ML335 (CID-53347902) Cat. No.: HY-12343 Cat. No.: HY-104005

Bioactivity: ML277(CID53347902) is a novel, potent and selective K(v)7.1 Bioactivity: ML335 is a selective activator of both TREK-1 and TREK-2. (KCNQ1) potassium channel activator with EC50 of 270 nM.

Purity: 98.14% 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, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

ML365 ML402 Cat. No.: HY-12345 Cat. No.: HY-104027

Bioactivity: ML365 is a novel selective small molecule inhibitor of Bioactivity: ML402 is a selective TREK-1 activator. TASK1(KCNK3) with IC50 of 4 nM(thallium influx fluorescent assay) and 16 nM(automated electrophysiology assay).

Purity: 98.38% Purity: 99.88% 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, 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 95

Myomodulin N-Acetylprocainamide Cat. No.: HY-P0268 (Acecainide; NAPA) Cat. No.: HY-B1109

Bioactivity: Myomodulin is a neuropeptide present in molluscs, insects, and Bioactivity: N-Acetylprocainamide is a class III antiarrhythmic, which gastropods. blocks K+ channels.

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, 100 mg

Naluzotan Naminidil (PRX 00023) Cat. No.: HY-14848 (BMS 234303-01) Cat. No.: HY-100276

Bioactivity: Naluzotan is a novel, potent, and selective amidosulfonamide Bioactivity: Naminidil is a cyanoguanidine KATP opener. 5-HT1A agonist with IC50 and Ki of appr 20 nM and 5.1 nM, used for the treatment of anxiety and depression; Also a weak + hERG K channel blocker, with IC 50 of 3800 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: 1 mg, 5 mg, 10 mg

Nicorandil Nigericin sodium salt (SG-75) Cat. No.: HY-B0341 (Sodium Nigericin) Cat. No.: HY-100381

Bioactivity: (SG-75) is potassium channel activator. Bioactivity: Nigericin sodium salt is an antibiotic from Streptomyces hygroscopicus that works by acting as an H +, K +, and Pb 2+ ionophore.

Purity: 99.94% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 50 mg

NS 11021 NS-1619 Cat. No.: HY-13103 Cat. No.: HY-12496

Bioactivity: NS 11021 is a potent and specific Ca2-activated Bioactivity: NS-1619 is a selective large conductance Ca2+-activated K+-channel activator. big-conductance K Channels (KCa1.1 channels) activator. NS 11021 at concentrations above 0.3 μM activates KCa1.1 in a concentration-dependent manner by parallelshifting the chan…

Purity: >98% Purity: 99.30% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size: 10mM x 1mL in DMSO, 5 mg, 10 mg

NS1643 NS309 Cat. No.: HY-16916 Cat. No.: HY-15416

Bioactivity: NS1643 is a potent human ether-a-go-go related gene (hERG) Bioactivity: NS309 is a positive modulator of small- and intermediate- KV11.1 channel activator (EC50 = 10.5 μM). IC50 value: Target: conductance Ca2+-activated K+ channels (KCa2 and KCa3.1 HERG activator in vitro: NS1643 enhanced the magnitude of channels); increases Ca2+ sensitivity. Displays no activity at wild-type hERG current in a concentration- and BK channels. voltage-dependent manner with an EC(50) of 10.4 microM at -10… Purity: 96.85% Purity: 98.76% 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, 10 mg, 50 mg

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

NS6180 P-1075 Cat. No.: HY-15707 Cat. No.: HY-108573

Bioactivity: NS6180 is a novel potent and selective KCa3.1 channel Bioactivity: P-1075 is a potent activator of sulfonylurea receptor inhibitor(IC50= 9 nM) prevents T-cell activation and 2-associated ATP-sensitive potassium channels (SUR2-KIR6), inflammation. with an EC50 value of 45 nM for SUR2B-K IR6 channel activation [1]. P-1075 also P1075 opens mitochondrial K(A… Purity: 99.99% 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

PAP-1 PD-118057 (5-(4-Phenoxybutoxy)psoralen) Cat. No.: HY-10015 Cat. No.: HY-108594

Bioactivity: PAP-1 is a selective inhibitor of Kv1.3, voltage-gated K+ Bioactivity: PD-118057 is a human ether-a-go-go-related gene (hERG) channel. PAP-1 (EC50=2 nM) potently inhibits human T effector channel activator that does not cause hERG blockade [1]. memory cell proliferation and delayed hypersensitivity. IC50 value: 2 nM (EC50) [1] in vitro: blocks Kv1.3 in a use-dependent manner, with a Hill coefficient of 2 and an EC50… Purity: 99.69% 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

PF 03716556 Phe-Met-Arg-Phe amide trifluoroacetate Cat. No.: HY-13100 Cat. No.: HY-P0249A

Bioactivity: PF 03716556 is a potent, and selective H +, K +-ATPase Bioactivity: Phe-Met-Arg-Phe amide trifluoroacetate is an activator of K +

antagonist, with a pIC 50 value of 6.009. current, with ED 50 of 23 nM in the peptidergic caudodorsal neurons.

Purity: >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 Water, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg

Phe-Met-Arg-Phe, amide monohydrate Cat. No.: HY-P0249 Cat. No.: HY-14290A

Bioactivity: Phe-Met-Arg-Phe, amide dose dependently (ED 50=23 nM) Bioactivity: Pinacidil monohydrate, an , is a potassium channel activator. activates a K + current in the peptidergic caudodorsal neurons.

Purity: >98% Purity: 99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 25 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg

Pirmenol hydrochloride hydrochloride monohydrate (Cl-845; (±)-Pirmenol hydrochlorid) Cat. No.: HY-100795A Cat. No.: HY-B1302

Bioactivity: Pirmenol hydrochloride inhibits IK.ACh by blocking Bioactivity: Quinidine hydrochloride monohydrate is a clinical anti-arrythmic drug which is also a potent blocker of K+ muscarinic receptors. The IC50 of Pirmenol for inhibition channel with an IC50 of 19.9 μM. of Carbachol-induced I K.ACh is 0.1 μM.

Purity: 97.20% Purity: 99.32% Clinical Data: Launched 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 100 mg

www.MedChemExpress.com 97

Quinine hydrochloride Cat. No.: HY-D0143 Cat. No.: HY-B0563B

Bioactivity: Quinine is an anti-malaria agent and also a potassium Bioactivity: Ropivacaine hydrochloride is an inhibitor of K2P (two-pore channel inhibitor with an IC50 of 169 μM. domain potassium channel) TREK-1 with an IC50 of 402.7 μM.

Purity: 99.59% Purity: 99.97% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g 10 mg, 50 mg

RPR-260243 Senicapoc Cat. No.: HY-16915 (ICA-17043) Cat. No.: HY-50694

Bioactivity: RPR-260243 is a novel activator of HERG; modifies HERG Bioactivity: Senicapoc (ICA-17043) is a potent and selective Gardos channel currents inhibited by dofetilide (IC50 = 58 nM); little effect 2+ blocker with IC50 value of 11 nM. It blocks Ca -induced on HERG current amplitude and no significant effects on rubidium flux from human RBCs with an IC value of 11 nM and steady-state activation parameters or on channel inactivation 50 processes. inhibits RBC dehydration with IC50 of 30 nM. Purity: 98.84% Purity: 99.83% 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, 50 mg 10 mg, 50 mg, 100 mg

SKA-121 SKA-31 Cat. No.: HY-107414 Cat. No.: HY-111655

Bioactivity: SKA-121 is a selective KCa3.1 activator. SKA-121 exhibits Bioactivity: SKA-31 is a potent potassium channel activator with EC50s of

EC50s of 109 nM and 4.4 μM for KCa3.1 and KCa2.3, 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, respectively. KCa2.1 and KCa2.3, respectively. SKA-31 potentiates endothelium-derived hyperpolarizing factor response and low…

Purity: 98.64% 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, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Tannic acid Cat. No.: HY-B2136 ((±)-Terfenadine; MDL-991) Cat. No.: HY-B1193

Bioactivity: Tannic acid is a novel hERG channel blocker with IC50 of 3.4 Bioactivity: Terfenadine is a potent open-channel blocker of hERG with a μM. mean IC50 of 204 nM.

Purity: 81.68% Purity: 98.26% 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

Tertiapin-Q Tetrandrine Cat. No.: HY-P1275 (NSC-77037d-Tetrandrine) Cat. No.: HY-13764

Bioactivity: -Q is a highly selective blocker of GIRK1/4 Bioactivity: Tetrandrine (NSC-77037) is a bis-benzyl-isoquinoline alkaloid, 2+ heterodimer and ROMK1 ( Kir1.1). which inhibits voltage-gated Ca current (ICa) and Ca 2+-activated K+ current.

Purity: 97.46% Purity: 99.90% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 100 mg, 250 mg

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

Tolbutamide TRAM-34 Cat. No.: HY-B0401 Cat. No.: HY-13519

Bioactivity: is a first generation potassium channel blocker, Bioactivity: TRAM-34 is a highly selective blocker of sulfonylurea oral hypoglycemic drug. Target: Potassium Channel intermediate-conductance calcium-activated K + channel ( Tolbutamide is an oral antihyperglycemic agent used for the IKCa1) ( Kd=20 nM). treatment of non-insulin-dependent diabetes mellitus (NIDDM). Tolbutamide act by stimulating β cells of the pancreas to… Purity: 99.96% Purity: 99.71% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 10 mg, 50 mg, 100 mg

U89232 Cat. No.: HY-U00173 (RSD1235) Cat. No.: HY-14182

Bioactivity: U-89232 appears to be a cardioselective KATP channel opener. Bioactivity: Vernakalant(RSD-1235) is an investigational mixed ion channel blocker that can terminate acute atrial fibrillation (AF) in humans at 2 to 5 mg/kg and may be more atrial-selective than available agents; in treatment of antiarrhythmic.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10 mg, 50 mg

Vernakalant Hydrochloride VU 0240551 (RSD1235 hydrochloride) Cat. No.: HY-14183 Cat. No.: HY-16689

Bioactivity: Vernakalant hydrochloride is a mixed voltage- and Bioactivity: VU 0240551 is a small molecule inhibitor of the neuronal K-Cl frequency-dependent Na+ and atria-preferred K+ channel cotransporter, KCC2 (IC50 = 560 nM for K+ uptake assay in KCC2-overexpressing cells). blocker. IC50 for block by Vernakalant of wild-type and mutant Kv1.5 channels Fractional block is 13.35±0.93 μM, 0.61±0… Purity: 99.33% Purity: 99.64% Clinical Data: Launched 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

VU0134992 VU0463271 Cat. No.: HY-122560 Cat. No.: HY-110110

Bioactivity: VU0134992 is a selective inward rectifier potassium (Kir) Bioactivity: VU0463271 is a potent KCC2 antagonist, with an IC50 of 61 nM. [1] channel Kir4.1 blocker with an IC50 of 0.97 µM .

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

VU0529331 VU591 Cat. No.: HY-112705 Cat. No.: HY-108585A

Bioactivity: VU0529331 is a modestly selective non-GIRK1-containing G Bioactivity: VU591 is a potent, selective renal outer medullary potassium

protein-gated, inwardly-rectifying, potassium channel ( channel (ROMK or Kir1.1) inhibitor, with an IC50 of 0.24 μM non-GIRK1/X) activator, with EC s of 5.1 µM and 5.2 µM for 50 [1]. GIRK2 and GIRK1/2 in HEK293 cells, respectively, a…

Purity: >98% Purity: 99.38% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 100 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg

www.MedChemExpress.com 99

VU591 hydrochloride XE 991 dihydrochloride Cat. No.: HY-108585 Cat. No.: HY-108577

Bioactivity: VU591 hydrochloride is a potent, selective renal outer Bioactivity: XE 991 dihydrochloride, a Kv7 (KCNQ) channels blocker, medullary potassium channel (ROMK or Kir1.1) inhibitor, with an potently inhibits Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.2 + [1] Kv7.3 (KCNQ3) channel, and M-current with IC s of 0.75 IC50 of 0.24 μM . 50 µM, 0.71 µM, 0.6 μM, and 0.98 µM, respectively [1]. Purity: 99.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg Size:

Y-26763 Y-27152 Cat. No.: HY-101069 Cat. No.: HY-108582

+ Bioactivity: Y-26763 is a K channel opener and active metabolite of Bioactivity: Y-27152, a prodrug of the K ATP (Kir6) channel opener [1] + Y-26763, is a long-acting K+ channel opener with less Y-27152 . Y-26763 is an ATP-sensitive K (K ATP) tachycardia: antihypertensive effects in hypertensive rats and channel activator [2]. dogs in conscious state [1] [2]. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg Size:

YM758 Cat. No.: HY-U00309

Bioactivity: YM758 is a “funny” I f current channel ( If channel) inhibitor.

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

100 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Proton Pump

Proton pump is an integral membrane protein that is capable of moving protons across a biological membrane. Mechanisms are based on conformational changes of the protein structure or on theQ cycle. In cell respiration, the proton pump uses energy to transport protons from the matrix of the mitochondrion to the inter-membrane space. It is an active pump, that generates a protonconcentration gradient across the inner mitochondrial membrane, because there are more protons outside the matrix than inside. The difference in pH and electric charge (ignoring differences inbuffer capacity) creates an electrochemical potential difference that works similar to that of a battery or energy storing unit for the cell. The process could also be seen as analogous to cycling uphill or charging a battery for later use, as it produces potential energy. The proton pump does not create energy, but forms a gradient that stores energy for later use.

www.MedChemExpress.com 101 Proton Pump Inhibitors & Modulators

(R)-Lansoprazole Bafilomycin A1 (Dexlansoprazole) Cat. No.: HY-13662B ((-)-Bafilomycin A1) Cat. No.: HY-100558

Bioactivity: (R)-Lansoprazole is a proton pump inhibitor which prevents the Bioactivity: Bafilomycin A1, a macrolide antibiotic isolated from the stomach from producing acid. Target: Proton Pump Lansoprazole Streptomyces species, is a specific inhibitor of sodium is sodium salt form of lansoprazole, lansoprazole, a vacuolar-type H+ ATPase (V-ATPase). Bafilomycin A1 inhibits substituted benzimidizole proton pump inhibitor, on autophagy [1]. and metabolism of has been… Purity: 98.0% Purity: 99.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 100 mg, 500 mg Size: 100u g

Bamaquimast Chebulinic acid (F 10126; L 0042) Cat. No.: HY-101427 Cat. No.: HY-N2033

Bioactivity: Bamaquimast is an inhibitor of proton pump extracted from Bioactivity: Chebulinic acid is a potent natural inhibitor of M. patent US2005165041, example 138. tuberculosis DNA gyrase, also can inhibit SMAD-3 phosphorylation, inhibit H+ K+-ATPase activity.

Purity: 98.79% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg 5 mg, 10 mg, 50 mg, 100 mg

Concanamycin A Esomeprazole magnesium (Antibiotic X 4357B; Concanamycin; X 4357B) Cat. No.: HY-N1724 ((S)-Omeprazole magnesium; (-)-Omeprazole magnesium) Cat. No.: HY-B1446

Bioactivity: Concanamycin A (Antibiotic X 4357B; Concanamycin; X 4357B) is Bioactivity: Esomeprazole magnesium is an inhibitor of H+, K+-ATPase, a macrolide antibiotic and a specific vacuolar type H+-ATPase effectively used in the research of upper intestinal disorder. (V-ATPase) inhibitor [1].

Purity: >98% Purity: 98.49% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size: 10mM x 1mL in DMSO, 50 mg

Esomeprazole magnesium salt Esomeprazole Magnesium trihydrate Cat. No.: HY-17021A ((S)-Omeprazole magnesium trihydrate) Cat. No.: HY-17022

Bioactivity: Esomeprazole magnesium salt is a proton pump inhibitor which Bioactivity: Esomeprazole Magnesium trihydrate is a proton pump inhibitor reduces acid secretion through inhibition of the H+ / K+ which reduces acid secretion through inhibition of the H+ / K+ ATPase in gastric parietal cells. IC50 value: Target: proton ATPase in gastric parietal cells. IC50 value: Target: proton pump Esomeprazole magnesium salt is a proton pump inhibitor pump Esomeprazole sodium (Nexium) is the S-isomer of and gastric antisecretory agent indicated for the short-term… omeprazole and acts as a proton pump inhibitor and gastric… Purity: >98% Purity: 95.0% Clinical Data: Launched Clinical Data: Launched Size: 5 mg, 10 mg Size: 50 mg, 100 mg, 200 mg, 500 mg

Esomeprazole potassium salt Esomeprazole sodium ((S)-Omeprazole potassium) Cat. No.: HY-17021B ((S)-Omeprazole sodium) Cat. No.: HY-17023

Bioactivity: Esomeprazole potassium salt is a proton pump inhibitor which Bioactivity: Esomeprazole sodium is a proton pump inhibitor which reduces reduces acid secretion through inhibition of the H+ / K+ acid secretion through inhibition of the H+ / K+ ATPase in ATPase in gastric parietal cells. gastric parietal cells. IC50 value: Target: proton pump Esomeprazole sodium (Nexium) is the S-isomer of omeprazole and acts as a proton pump inhibitor and gastric antisecretory… Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 50 mg, 100 mg Size: 5 mg, 10 mg, 50 mg

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

Ilaprazole Lansoprazole (IY-81149) Cat. No.: HY-101664 (AG-1749) Cat. No.: HY-13662

Bioactivity: Ilaprazole (IY-81149) is a proton pump inhibitor; inhibits Bioactivity: Lansoprazole(AG 1749) is a proton pump inhibitor which + + prevents the stomach from producing acid. H /K -ATPase with an IC50 of 6.0 μM.

Purity: 98.0% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg 1 g, 5 g

Lansoprazole sodium Linaprazan (AG-1749 sodium) Cat. No.: HY-13662A (AZD0865) Cat. No.: HY-100412

Bioactivity: Lansoprazole sodium(AG-1749) is a proton pump inhibitor which Bioactivity: Linaprazan (AZD0865) inhibits gastric H+,K+-ATPase by prevents the stomach from producing acid. K+-competitive binding. (IC50: 1.0 ± 0.2 μM) It is a acid-suppressing agents with rapid onset of action and potent acid inhibition. In vitro: Linaprazan can inhibit the final step in acid secretion. Linaprazanreduced porcine renal… Purity: >98% Purity: 98.89% Clinical Data: Launched Clinical Data: Phase 2 Size: 1 g, 5 g Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Omeprazole Omeprazole D3 (H 16868) Cat. No.: HY-B0113 (H 16868 D3) Cat. No.: HY-B0113S

Bioactivity: Omeprazole (H 16868) is a proton pump inhibitor used in the Bioactivity: Omeprazole D3 (H 16868 D3) is deuterium labeled Omeprazole, treatment of dyspepsia. which is a proton pump inhibitor used in the treatment of dyspepsia.

Purity: 97.06% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg 100 mg, 500 mg

Pantoprazole Pantoprazole sodium (BY1023; SKF96022) Cat. No.: HY-17507 (BY1023 (sodium); SKF96022 (sodium)) Cat. No.: HY-17507A

Bioactivity: Pantoprazole(SKF96022; Protonix) is a proton pump inhibitor Bioactivity: Pantoprazole sodium salt(SKF96022; Protonix) is a proton pump drug used for short-term treatment of erosion and ulceration inhibitor drug used for short-term treatment of erosion and of the esophagus caused by gastroesophageal reflux disease. ulceration of the esophagus caused by gastroesophageal reflux IC50 value: Target: proton pump inhibitor disease. IC50 value: Target: proton pump inhibitor

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

Pantoprazole sodium hydrate Picoprazole (BY1023 (sodium hydrate); SKF96022 (sodium hydrate)) Cat. No.: HY-17507B Cat. No.: HY-15384

Bioactivity: Pantoprazole sodium hydrate is a proton pump inhibitor drug Bioactivity: Picoprazole is a specific inhibitor of H+/K+-ATPase with used for short-term treatment of erosion and ulceration of the IC50 of 3.1±0.4 μM. esophagus caused by gastroesophageal reflux disease. IC50 value: Target: proton pump inhibitor

Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 100 mg, 500 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

www.MedChemExpress.com 103

Pumaprazole Rabeprazole (BY-841) Cat. No.: HY-19223 (LY307640) Cat. No.: HY-B0656

Bioactivity: Pumaprazole is a reversible proton pump antagonist. Bioactivity: Rabeprazole is an antiulcer drug in the class of proton pump inhibitors.

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

Rabeprazole sodium S3337 (LY307640 sodium) Cat. No.: HY-B0656A Cat. No.: HY-U00222

Bioactivity: Rabeprazole sodium(LY307640 sodium) is an antiulcer drug in Bioactivity: S3337 is an H +, K +-ATPase inhibitor. the class of proton pump inhibitors.

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 10 mg, 50 mg

SCH28080 SKF96067 Cat. No.: HY-103261 Cat. No.: HY-U00042

Bioactivity: SCH28080 inhibits gastric H+/K+-ATPase by K+-competitive Bioactivity: SKF96067 is a reversible inhibitor of the gastric + + binding, with an IC50 value of 20 nM in rabbit microsomal H /K -ATPase. membranes [1]. Antisecretory and cytoprotective activities [2]. Purity: 99.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

Soraprazan Tegoprazan (BYK61359) Cat. No.: HY-100414 Cat. No.: HY-17623

Bioactivity: Soraprazan is a reversible, and fast-acting inhibitor of Bioactivity: Tegoprazan, a potassium-competitive acid blocker, is a potent, gastric H+/K+ ATPase. oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and

motility, with IC50 values ranging from 0.29-0.52 μM … Purity: 99.02% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Tenatoprazole sodium Vonoprazan (Tenatoprazole sodium salt) Cat. No.: HY-17421A (TAK-438 (free base)) Cat. No.: HY-100007

Bioactivity: Tenatoprazole sodium (TU-199 sodium) is a proton pump Bioactivity: Vonoprazan (TAK-438 free base) is an orally active + + + inhibitor; inhibits hog gastric H /K -ATPase with an IC50 potassium-competitive acid blocker which inhibits H , K + of 6.2 μM. -ATPase activity with an IC50 of 19 nM.

Purity: >98% Purity: 99.33% 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

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

Vonoprazan Fumarate Pyrithione (TAK-438) Cat. No.: HY-15295 Cat. No.: HY-B0572

Bioactivity: Vonoprazan Fumarate (TAK-438) is an orally active Bioactivity: Zinc Pyrithione is an antifungal and antibacterial agent potassium-competitive acid blocker which inhibits H +, K disrupting membrane transport by blocking the proton pump. Target: Proton Pump Zinc pyrithione is considered as a +-ATPase activity with an IC of 19 nM. 50 coordination complex of zinc. The pyrithione ligands, which are formally monoanions, are chelated to Zn 2+ via oxygen and… Purity: 99.97% 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 g, 5 g

www.MedChemExpress.com 105 SGLT Sodium-dependent glucose cotransporters

SGLT (Sodium-dependent glucose cotransporters) are a family of glucose transporter found in the intestinal mucosa (enterocytes) of the small intestine (SGLT1) and the proximal tubule of the nephron (SGLT2 in PCT and SGLT1 in PST). SGLT contribute torenal glucose reabsorption. In the kidneys, 100% of the filtered glucose in the glomerulus has to be reabsorbed along the nephron (98% in PCT, via SGLT2). In case of too high plasma glucose concentration (hyperglycemia), glucose is excreted in urine (glucosuria); because SGLT are saturated with the filtered monosaccharide. Glucose is never secreted by the nephron. There are two most well known members of SGLT family are SGLT1 and SGLT2, which are members of the SLC5A gene family. Inhibition of SGLT2 leads to a reduction in blood glucose levels. Therefore, SGLT2 inhibitors have potential use in the treatment of type II diabetes.

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

Bexagliflozin Canagliflozin (EGT1442; EGT0001442; THR-1442) Cat. No.: HY-17604 (JNJ 24831754ZAE; JNJ 28431754; JNJ 28431754AAA; TA 7284)Cat. No.: HY-10451

Bioactivity: Bexagliflozin is a potent and selective SGLT2 inhibitor with Bioactivity: Canagliflozin (TA 7284) is a selective SGLT2 inhibitor with IC50 value of 5.6 μM /2 nM in SGLT1 /SGLT2 respectively. IC50s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and target: SGLT2 IC50: 5.6 μM (SGLT1)/ 2 nM (SGLT2) 1) In normal hSGLT2 in CHOK cells, respectively [1]. rats and dogs a saturable urinary glucose was produced with an ED50 of 0.38 and 0.09 mg/kg, respectively. 2)… Purity: 99.48% Purity: 99.61% Clinical Data: Phase 3 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Canagliflozin hemihydrate (JNJ 24831754ZAE (hemihydrate); JNJ Dapagliflozin 28431754 (hemihydrate); …) Cat. No.: HY-I0383 (BMS-512148) Cat. No.: HY-10450

Bioactivity: Canagliflozin hemihydrate (JNJ28431754 hemihydrate; TA-7284 Bioactivity: Dapagliflozin (BMS-512148) is a sodium-glucose co-transporter

hemihydrate) is a selective SGLT2 inhibitor with IC50s of 2 2 ( SGLT2) inhibitor for the treatment of type 2 diabetes. nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively [1]. Purity: 99.95% Purity: 99.85% 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, 500 mg 5 mg, 10 mg, 50 mg, 100 mg

Dapagliflozin ((2S)-1,2-propanediol, hydrate) Empagliflozin (BMS-512148 (2S)-1,2-propanediol, hydrate) Cat. No.: HY-10450A (BI 10773) Cat. No.: HY-15409

Bioactivity: Dapagliflozin (2S)-1,2-propanediol, hydrate is the Bioactivity: Empagliflozin is a selective sodium glucose cotransporter-2 (

S-enantiomer of Dapagliflozin 1,2-propanediol, hydrate. SGLT-2) inhibitor with an IC50 of 3.1 nM for human SGLT-2. Dapagliflozin inhibits sodium/glucose cotransporter 2 ( SGLT2), which results in excretion of glucose into the uri…

Purity: 99.99% Purity: 99.90% Clinical Data: Phase 4 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, 200 mg, 500 mg, 1 g, 5 g, 10 g

Ertugliflozin Ertugliflozin L-pyroglutamic acid (PF-04971729) Cat. No.: HY-15461 (PF-04971729 L-pyroglutamic acid) Cat. No.: HY-15461A

Bioactivity: Ertugliflozin (PF-04971729) is a potent, selective and orally Bioactivity: Ertugliflozin (PF-04971729) L-pyroglutamic acid is a potent, active inhibitor of the sodium-dependent glucose cotransporter selective and orally active inhibitor of the sodium-dependent [1] glucose cotransporter 2 (SGLT2), with an IC of 0.877 nM 2 (SGLT2), with an IC 50 of 0.877 nM for h-SGLT2 . A drug 50 [1] for the treatment of type 2 diabetes mellitus [2]. for h-SGLT2 . A drug for the treatment of type 2 diabe… Purity: 99.80% Purity: 99.98% 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 5 mg, 10 mg, 50 mg

HSK0935 Ipragliflozin (HSK-0935; HSK 0935) Cat. No.: HY-101782 (ASP1941) Cat. No.: HY-14894

Bioactivity: HSK0935 is a potent, highly selective and orally available Bioactivity: Ipragliflozin (ASP1941) is a highly potent and selective SGLT2

SGLT2 inhibitor with an IC50 of 1.3 nM. Antihyperglycemic inhibitor with IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6. IC50 value: 2.8 nM [1][2] Target: SGLT2 in activities [1]. vitro: Ipragliflozin potently and selectively inhibited human, rat, and mouse SGLT2 at nanomolar ranges and exhibited… Purity: >98% Purity: 99.86% Clinical Data: No Development Reported Clinical Data: Phase 4 Size: 250 mg, 500 mg Size: 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

www.MedChemExpress.com 107

Ipragliflozin L-Proline Licogliflozin Cat. No.: HY-14894A (LIK066) Cat. No.: HY-109092

Bioactivity: Ipragliflozin (L-) is a highly potent and selective Bioactivity: Licogliflozin is a sodium glucose cotransporter ( SGLT1 and

SGLT2 inhibitor with an IC50 of 2.8 nM; little and NO potency SGLT2) inhibitor. for SGLT1/3/4/5/6.

Purity: >98% Purity: 98.53% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg Size: 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Phloretin Phlorizin (NSC 407292; RJC 02792) Cat. No.: HY-N0142 (Floridzin; NSC 2833) Cat. No.: HY-N0143

Bioactivity: Phloretin(NSC 407292; RJC 02792) is a dihydrochalcone, a type Bioactivity: Phlorizin is a non-selective SGLT inhibitor with Kis of 300 of natural . Phloretin inhibits the active transport of and 39 nM for hSGLT1 and hSGLT2, respectively. Phlorizin is glucose into cells by SGLT1 and SGLT2. also a Na+/K+-ATPase inhibitor.

Purity: 99.70% Purity: 95.33% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 250 mg, 500 mg 1 g, 5 g

SGL5213 SGLT inhibitor-1 Cat. No.: HY-114308 Cat. No.: HY-112807

Bioactivity: SGL5213 is a potent, oral active and low-absorbable Bioactivity: SGLT inhibitor-1 is a potent dual inhibitor of sodium sodium-dependent glucose cotransporter 1 (SGLT1) glucose co-transporter proteins (SGLTs), inhibits hSGLT1 and inhibitor, with IC values of 29 nM and 20 nM for hSGLT1 and [1] 50 hSGLT2 with IC50s of 43 nM and 9 nM, respectively . hSGLT2, respectively. SGL5213 has potential to treat typ…

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

Sotagliflozin Tofogliflozin (LX-4211; LP-802034) Cat. No.: HY-15516 (CSG452) Cat. No.: HY-14902

Bioactivity: Sotagliflozin (LX-4211) is a potent dual SGLT2/1 inhibitor. Bioactivity: Tofogliflozin(CSG-452) is a potent and highly specific Antidiabetic agents. sodium/glucose cotransporter 2(SGLT2) inhibitor with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2.

Purity: 99.99% Purity: >98% Clinical Data: Phase 3 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg

Tofogliflozin hydrate Velagliflozin (CSG-452 hydrate) Cat. No.: HY-13413 Cat. No.: HY-109018

Bioactivity: Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly Bioactivity: Velagliflozin is an orally available sodium-glucose specific sodium/glucose cotransporter 2(SGLT2) inhibitor with cotransporter 2 ( SGLT2) inhibitor, with anti-diabetic Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse activity. SGLT2. IC50 value: 2.9/14.9/6.4 nM(human/rat/mouse SGLT2) [1] Target: SGLT2 inhibitor in vitro: Tofogliflozin competitively… Purity: 99.41% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 5 mg, 10 mg, 50 mg

108 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Sodium Channel Na channels;Na+ channels

Sodium channels are integral membrane proteins that form ion channels, conducting sodium ions (Na +) through a cell's plasma membrane. They are classified according to the trigger that opens the channel for such ions, i.e. either a voltage-change (Voltage-gated, voltage-sensitive, or voltage-dependent sodium channel also called VGSCs or Nav channel) or a binding of a substance (a ligand) to the channel (ligand-gated sodium channels). In excitable cells such as neurons, myocytes, and certain types of glia, sodium channels are responsible for the rising phase of action potentials. Voltage-gated Na+ channels can exist in any of three distinct states: deactivated (closed), activated (open), or inactivated (closed). Ligand-gated sodium channels are activated by binding of a ligand instead of a change in membrane potential.

www.MedChemExpress.com 109 Sodium Channel Inhibitors & Modulators

(+)-Kavain (-)-Sparteine sulfate pentahydrate Cat. No.: HY-B1671 ((-)-Lupinidine (sulfate pentahydrate)) Cat. No.: HY-B1304

Bioactivity: (+)-Kavain, a main kavalactone extracted from Piper Bioactivity: (-)-Sparteine sulfate pentahydrate ((-)-Lupinidine sulfate methysticum, has anticonvulsive properties, attenuating pentahydrate) is a class 1a antiarrhythmic agent and a sodium vascular smooth muscle contraction through interactions with channel blocker. It is an alkaloid, can chelate the bivalents voltage-dependent Na + and Ca 2+ channels [1]. (+)-Kav… calcium and magnesium.

Purity: 99.98% Purity: 98.0% 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

A-803467 Ajmaline Cat. No.: HY-11079 (Cardiorythmine; (+)-Ajmaline) Cat. No.: HY-B1167

Bioactivity: A 803467 is a selective Nav1.8 with an Bioactivity: Ajmaline is an alkaloid that is class Ia antiarrhythmic agent. IC50 of 8 nM; over 100-fold more selective . human Nav1.2, 1.3, 1.5 and 1.7.

Purity: 97.51% Purity: 99.31% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 50 mg, 100 mg

AM-2099 Cat. No.: HY-100727 (MK-870) Cat. No.: HY-B0285

Bioactivity: AM-2099 is a potent and selective inhibitor of voltage-gated Bioactivity: Amiloride is a relatively selective inhibitor of the

sodium channel Nav1.7 with an IC50 of 0.16 μM for human epithelial sodium channel (ENaC), used in the management Nav1.7. of hypertension and congestive heart failure.

Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Amiloride hydrochloride Amiloride hydrochloride dihydrate (MK-870 hydrochloride) Cat. No.: HY-B0285A (MK-870 hydrochloride dihydrate) Cat. No.: HY-B0285B

Bioactivity: Amiloride hydrochloride (MK-870 hydrochloride) is an epithelial Bioactivity: Amiloride hydrochloride dihydrate is an inhibitor of both sodium channel (ENaC) inhibitor and a competitive inhibitor Epithelial sodium channel ( ENaC) and urokinase-type of Urokinase-type plasminogen activator ( uPA). plasminogen activator receptor ( uTPA).

Purity: 98.0% Purity: 98.56% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 100 mg

Amitriptyline hydrochloride hydrochloride Cat. No.: HY-B0527A (Benzylamiloride hydrochloride) Cat. No.: HY-B1546A

Bioactivity: Hydrochloride is a Bioactivity: Benzamil hydrochloride is a specific blocker of sodium dibenzocycloheptene-derivative (TCA). channel ( ENaC).

Purity: 99.64% Purity: 99.46% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 1 g, 5 g 5 mg, 10 mg, 50 mg, 100 mg

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

Benzocaine BI 01383298 Cat. No.: HY-Y0258 Cat. No.: HY-124738

Bioactivity: shares a common receptor with all other local Bioactivity: BI 01383298 is a potent inhibitor of the sodium-citrate (LAs) in the voltage-gated Na+ channel, with an co-transporter (SLC13A5) that is highly expressed in the liver [1]. IC50 of 0.8 mM tested with a potential of +30 mV.

Purity: 99.98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 g, 10 g 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

BI-9627 Bulleyaconitine A Cat. No.: HY-18071 Cat. No.: HY-N0239

Bioactivity: BI-9627 is a sodium−hydrogen exchanger isoform 1 (NHE1) Bioactivity: Bulleyaconitine A is an analgesic and antiinflammatory drug [1] isolated from Aconitum plants; has several potential targets, inhibitor with an EC50 of 31 nM . including voltage-gated Na+ channels.

Purity: 99.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 5 mg

Carbamazepine Cariporide (CBZ; NSC 169864) Cat. No.: HY-B0246 (HOE-642) Cat. No.: HY-19693

Bioactivity: , a sodium channel blocker, is an anticonvulsant Bioactivity: Cariporide (HOE-642) is a selective Na+/H+ exchange drug. Target: Sodium channel Carbamazepine inhibits the inhibitor. binding of [3H]batrachotoxinin A 20-α-benzoate (BTX-B) to a receptor site of voltage-sensitive sodium channel with IC50 of 131 μM, to decrease the activation of sodium channel ion flux… Purity: 99.35% Purity: 98.57% 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, 50 mg, 100 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

Dibucaine Dibucaine hydrochloride () Cat. No.: HY-B0552 (Cinchocaine hydrochloride) Cat. No.: HY-B0552A

Bioactivity: Dibucaine is a local anesthetic of the amide type now Bioactivity: Dibucaine Hydrochloride is a local anesthetic of the amide generally used for surface anesthesia. type now generally used for surface anesthesia.

Purity: 99.81% Purity: 99.67% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 g, 10 g 5 g, 10 g

www.MedChemExpress.com 111

Dyclonine hydrochloride EIPA (Dyclocaine hydrochloride) Cat. No.: HY-B0364A (L593754; MH 12-43; Ethylisopropylamiloride) Cat. No.: HY-101840

Bioactivity: Dyclonine is an oral anaesthetic found in Sucrets, an over the Bioactivity: EIPA is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. counter throat lozenge. EIPA also inhibits Na+/H+-exchanger ( NHE) and macropinocytosis.

Purity: 99.72% Purity: 99.73% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 g, 10 g 5 mg, 10 mg

EIPA hydrochloride (L593754 hydrochloride; MH 12-43 Eleclazine hydrochloride hydrochloride; Ethylisopropylamiloride hydrochloride) Cat. No.: HY-101840A (GS 6615 hydrochloride) Cat. No.: HY-16738A

Bioactivity: EIPA hydrochloride (L593754 hydrochloride) is a TRPP3 channel Bioactivity: Eleclazine hydrochloride is a novel late Na+ current inhibitor [1] with IC50 value of 0.7 uM. target: Na+ current. IC50: 0.7 uM. inhibitor with an IC50 of 10.5 μM . EIPA also inhibits In vitro: Eleclazine hydrochloride inhibits ATX-II enhanced + + [2] [3] Na /H -exchanger ( NHE) and macropinocytosis . late INa in ventricular myocytes, shorten the ATX-II induced prolongation of APD, MAPD, QT interval, and decreased… Purity: >98% Purity: 99.47% 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 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Eniporide hydrochloride (EMD-96785 hydrochloride) Cat. No.: HY-106150B (BIA 2-093) Cat. No.: HY-B0703

Bioactivity: Eniporide hydrochloride (EMD-96785 hydrochloride) is a potent Bioactivity: Eslicarbazepine acetate, an antiepileptic drug, is a dual a Na+/H+ exchange inhibitor. dual Inhibitor of β-Secretase and voltage-gated sodium channel.

Purity: 99.31% 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 10 mg, 50 mg, 100 mg, 500 mg

Flecainide acetate FR183998 free base (R-818) Cat. No.: HY-17429 Cat. No.: HY-100302

Bioactivity: acetate (R-818) is a class 1C antiarrhythmic drug Bioactivity: FR183998 free base is a potent Na+/H+-exchange inhibitor, especially used for the management of supraventricular with IC50s of 0.3 nM, 3.1 nM and 6.5 nM by measurement of pH i arrhythmia; works by blocking the Nav1.5 sodium channel in the change in rat lymphocytes, rat and human platelets, heart, causing prolongation of the . respectively. Purity: 99.65% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 1 mg, 5 mg, 10 mg 10 mg, 50 mg, 100 mg

Funapide Ginsenoside Rg3 (TV 45070; XEN402) Cat. No.: HY-16723 (20(S)-Ginsenoside-Rg3; Rg3; S-Ginsenoside Rg3) Cat. No.: HY-N0603

Bioactivity: (TV 45070; XEN402) is a potent Sodium Channel Bioactivity: Ginsenoside Rg3 is the main component of Red ginseng. Nav1.7 inhibitor. Ginsenoside Rg3 inhibits Na+ and hKv1.4 channel with IC

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% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg

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

GNE-131 GS967 Cat. No.: HY-112279 Cat. No.: HY-12593

Bioactivity: GNE-131 is a potent and selective inhibitor of human sodium Bioactivity: GS967 (GS-458967) is a potent, and selective inhibitor of

channel NaV1.7, with an IC50 of 3 nM. cardiac late sodium current (late INa ) with IC50 values of 0.13 and 0.21 μM for ventricular myocytes and isolated , respectively.

Purity: >98% Purity: 99.96% 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, 200 mg

ICA-121431 Cat. No.: HY-16787 (LTG; BW430C) Cat. No.: HY-B0495

Bioactivity: ICA-121431 is a nanomolar potent small molecule Nav1.7 channel Bioactivity: Lamotrigine(BW430C) is a novel anticonvulsant drug for inhibitor with IC50 of 19 nM for rat Nav1.7, but no inhibition inhibition of 5-HT and sodium channel Target: Sodium Channel on human, monkey and dog Nav1.7. Lamotrigine stabilises presynaptic neuronal membranes by blockade of voltage-dependent sodium channels, thus preventing the release of excitatory neurotransmitters, particularly… Purity: 98.29% Purity: 99.94% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 1 g, 5 g

Lidocaine hydrochloride (Lignocaine) Cat. No.: HY-B0185 (Lignocaine hydrochloride) Cat. No.: HY-B0185A

Bioactivity: Lidocaine, an amide local anesthetic, has anti-inflammatory Bioactivity: Lidocaine Hcl salt, an amide local anesthetic, has properties in vitro and in vivo, possibly due to an anti-inflammatory properties in vitro and in vivo, possibly attenuation of pro-inflammatory cytokines, intracellular due to an attenuation of pro-inflammatory cytokines, adhesion molecule-1 (ICAM-1), and reduction of neutrophils intracellular adhesion molecule-1 (ICAM-1), and reduction of influx. neutrophils influx. Purity: 99.52% Purity: 99.95% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 g, 10 g 5 g, 10 g

Mepivacaine hydrochloride Metaflumizone Cat. No.: HY-B0517A (BAS-320I) Cat. No.: HY-116448

Bioactivity: is a tertiary amine used as a local anesthetic. Bioactivity: Metaflumizone is a insecticide, acts as a potent sodium channel blocker [1].

Purity: 99.83% Purity: 96.09% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 100 mg, 500 mg

Meticrane hydrochloride Cat. No.: HY-B0908 (KOE-1173 (hydrochloride)) Cat. No.: HY-A0093

Bioactivity: Meticrane is a diuretic. Meticrane inhibits the reabsorption Bioactivity: Mexiletine (hydrochloride) (KOE-1173 (hydrochloride)) is a of sodium and chloride ions in the distal convoluted tubule. non-selective voltage-gated sodium channel blocker; Class IB Meticrane is used to treat essential hypertension. anti-arrhythmic compound.

Purity: 98.79% Purity: 99.96% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 100 mg, 500 mg

www.MedChemExpress.com 113

Moricizine Myomodulin (Moracizine) Cat. No.: HY-B0615 Cat. No.: HY-P0268

Bioactivity: Moricizine is an antiarrhythmia agent used primarily for Bioactivity: Myomodulin is a neuropeptide present in molluscs, insects, and ventricular rhythm disturbances. gastropods.

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

Nav1.7 inhibitor NaV1.7 inhibitor-1 Cat. No.: HY-13985 Cat. No.: HY-119934

Bioactivity: Nav1.7 inhibitor is a potent Nav1.7 inhibitor. IC50 value: Bioactivity: NaV1.7 inhibitor-1 is an efficacious voltage-gated sodium Target: Nav1.7 Preparation of derivatives as channel (NaV) 1.7 inhibitor with an IC50 of 0.6 nM for Nav1.7 inhibitors By Brown, Alan Daniel; Rawson, David James; hNaV1.7, exhibits 80-fold selectivity versus hNaV1.5 [1]. Storer, Robert Ian; Swain, Nigel Alan From PCT Int. Appl. (2012), WO 2012007868 A2 20120119. Purity: 99.87% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 500 mg, 100 mg, 250 mg 5 mg, 10 mg, 50 mg, 100 mg

Nav1.7-IN-2 Nav1.7-IN-3 Cat. No.: HY-19366 Cat. No.: HY-101789

Bioactivity: Nav1.7-IN-2 is an inhibitor of voltage-gated sodium channels Bioactivity: Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated (Nav), in particular Nav 1.7, with IC50 of 80 nM. sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration [1].

Purity: >98% 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, 100 mg

NHE3-IN-1 Nicainoprol Cat. No.: HY-100325 (RU-42924) Cat. No.: HY-100572

Bioactivity: NHE3-IN-1 is a sodium/proton exchanger type 3 (NHE-3) Bioactivity: Nicainoprol is a fast- sodium-channel blocking drug, which inhibitor extracted from patent WO 2011019784 A1. is a potent antiarrhythmic agent.

Purity: >98% Purity: 99.48% 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

Oxcarbazepine PF 04531083 (GP 47680) Cat. No.: HY-B0114 Cat. No.: HY-105283

Bioactivity: (GP 47680) inhibits the binding of [3H]BTX to Bioactivity: PF 04531083 is a selective NaV1.8 blocker, and used for the sodium channels with IC 50 of 160 μM and also inhibits the research of neuropathic/inflammatory pain.

influx of 22Na+ into rat brain synaptosomes with IC 50 about 100 μM. Purity: 99.82% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 10 mg, 50 mg

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

PF 05089771 PF-01247324 Cat. No.: HY-12883 Cat. No.: HY-101383

Bioactivity: PF 05089771 is a Nav1.7 channel blocker extracted from patent Bioactivity: PF-01247324 is a selective and orally bioavailable Nav1.8 WO/2010/079443 A1, compound example 788, has an IC50 of 8.6 channel blocker with an IC of 196 nM for recombinant human nM. 50 Na v1.8 channel.

Purity: 99.32% Purity: 99.42% 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, 25 mg, 50 mg, 100 mg

PF-05241328 PF-06305591 Cat. No.: HY-103623 Cat. No.: HY-114301

Bioactivity: PF-05241328 is a potent and selective inhibitor of human Bioactivity: PF-06305591 is a potent and highly selective voltage gated

Nav1.7 voltage-dependent sodium channels (Nav1.7), with an sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An IC of 31 nM. 50 excellent preclinical in vitro ADME and safety profile [1].

Purity: >98% Purity: 99.0% 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

PF-06869206 Cat. No.: HY-112065 (5,5-Diphenylhydantoin) Cat. No.: HY-B0448

Bioactivity: PF-06869206 is an orally bioavailable selective inhibitor of Bioactivity: Phenytoin is an inactive voltage-gated sodium channel the sodium-phosphate cotransporter NaPi2a ( SLC34A1) with an stabilizer.

IC 50 of 380 nM.

Purity: >98% Purity: 99.91% 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 1 g, 5 g

Phenytoin sodium D7 hydrochloride (5,5-Diphenylhydantoin sodium salt) Cat. No.: HY-B0448A (SA-79 (D7 hydrochloride)) Cat. No.: HY-B0432AS

Bioactivity: Phenytoin sodium is an inactive voltage-gated sodium channel Bioactivity: Propafenone (D7 hydrochloride) (SA-79 (D7 hydrochloride)) is stabilizer. the deuterium labeled Propafenone, which is a classic anti-arrhythmic medication.

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 1 g, 5 g

Propafenone hydrochloride Proparacaine Hydrochloride (SA-79 (hydrochloride)) Cat. No.: HY-B0432A ( Hydrochloride) Cat. No.: HY-66012

Bioactivity: Propafenone (hydrochloride) (SA-79 (hydrochloride)) is a class Bioactivity: Proparacaine Hydrochloride is a voltage-gated sodium channels of anti-arrhythmic medication, which treats illnesses antagonist with ED50 of 3.4 mM. associated with rapid heart beats such as atrial and ventricular arrhythmias.

Purity: 99.70% Purity: 99.56% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 100 mg

www.MedChemExpress.com 115

Propoxycaine hydrochloride Ranolazine Cat. No.: HY-B1243 (CVT 303; RS 43285-003) Cat. No.: HY-B0280

Bioactivity: hydrochloride is the hydrochloride salt form of Bioactivity: Ranolazine is an antianginal medication. Propoxycaine, a para-aminobenzoic acid ester with local anesthetic activity. Target: sodium channel Propoxycaine binds to and inhibits voltage-gated sodium channels, thereby inhibiting the ionic flux required for the initiation and… Purity: 99.98% 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

Ranolazine dihydrochloride Raxatrigine (CVT 303 (dihydrochloride); RS 43285) Cat. No.: HY-17401 (GSK-1014802; CNV1014802) Cat. No.: HY-12796

Bioactivity: Ranolazine dihydrochloride (RS-43285) is an antianginal agent Bioactivity: Raxatrigine (GSK-1014802) is a novel small molecule with antiarrhythmic properties that achieves its effects via a state-dependent sodium channel blocker; Nav1.7 sodium channel novel mechanism of action (inhibition of the late phase of the inhibitor. inward sodium current), without affecting heart rate or blood pressure (BP). IC50 value: Target: sodium-dependent calcium… Purity: 99.92% Purity: 99.47% Clinical Data: Launched Clinical Data: Phase 2 Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 100 mg, 200 mg, 500 mg, 1 g, 5 g 5 mg, 10 mg, 50 mg, 100 mg

Raxatrigine hydrochloride Riluzole (GSK-1014802 hydrochloride; CNV1014802 (hydrochloride)) Cat. No.: HY-12796A (PK 26124) Cat. No.: HY-B0211

Bioactivity: Raxatrigine hydrochloride (GSK-1014802 hydrochloride) is a Bioactivity: Riluzole is an anticonvulsant drug and belongs to the family novel small molecule state-dependent sodium channel blocker; of use-dependent Na+ channel blocker which can also inhibit Nav1.7 sodium channel inhibitor. GABA uptake with an IC50 of 43 μM.

Purity: 98.69% Purity: 99.83% Clinical Data: Phase 2 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 50 mg, 100 mg, 500 mg, 1 g

Riluzole hydrochloride Rimeporide (PK 26124 hydrochloride) Cat. No.: HY-B0211A (EMD-87580) Cat. No.: HY-19273

Bioactivity: Riluzole hydrochloride is an anticonvulsant drug and belongs Bioactivity: Rimeporide (EMD-87580) is a potent and selective inhibitor of to the family of use-dependent Na+ channel blocker which can the Na+/H+ exchanger (NHE-1).

also inhibit GABA uptake with an IC50 of 43 μM.

Purity: 99.94% Purity: 98.77% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 500 mg 1 mg, 5 mg

Rimeporide hydrochloride Ropivacaine hydrochloride monohydrate (EMD-87580 hydrochloride) Cat. No.: HY-19273A Cat. No.: HY-B0563A

Bioactivity: Rimeporide hydrochloride (EMD-87580 hydrochloride) is a potent Bioactivity: Ropivacaine hydrochloride monohydrate is an anaesthetic agent and selective inhibitor of the Na+/H+ exchanger (NHE-1). and blocks impulse conduction in nerve fibres through inhibiting sodium ion influx reversibly. Target: Sodium Channel Ropivacaine is a new long-acting local anesthetic, with vasoconstrictive properties. Ropivacaine given epidurally… Purity: >98% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10mM x 1mL in Water, 10 mg, 50 mg

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

Sipatrigine Sodium Channel inhibitor 1 (619C89; BW 619C89) Cat. No.: HY-108335 Cat. No.: HY-15736

Bioactivity: Sipatrigine, a neuroprotective agent, is a glutamate release Bioactivity: Sodium Channel inhibitor1, one of inhibitor, voltage-dependent sodium channel and calcium 3-Oxoisoindoline-1-carboxamides, is a novel and selective channel inhibitor, penetrating the central nervous system. Has voltage-gated sodium channel for pain treatment. potential to treat focal cerebral ischemia and stroke [1]

Purity: 99.0% 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 5 mg

Sodium Channel inhibitor 2 Sodium ionophore III Cat. No.: HY-100257 (ETH2120) Cat. No.: HY-101109

Bioactivity: Sodium Channel inhibitor 2 is a sodium channel blocker Bioactivity: Sodium ionophore III (ETH2120) is a Na+ ionophore suitable extracted from patent WO 2004011439 A2, compound 3c. for the assay of sodium activity in blood, plasma, serum. etc.

Purity: >98% Purity: 98.07% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 10 mg, 50 mg, 100 mg, 200 mg

Tenapanor Tetracaine (AZD1722; RDX5791) Cat. No.: HY-15991 (Amethocaine) Cat. No.: HY-A0079

Bioactivity: Tenapanor is an inhibitor of the Na+/H+ exchanger NHE3 with Bioactivity: Tetracaine is a topical local anesthetic for the eyes; works by interfering with entry of sodium ions into nerve cells. IC50 values of 5 and 10 nM against human and Rat NHE3, respectively.

Purity: 98.80% Purity: 98.03% Clinical Data: Phase 3 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 1 g, 5 g

Triamterene D5 Cat. No.: HY-B0575 Cat. No.: HY-B0575S

Bioactivity: Triamterene blocks epithelial Na+ channel (ENaC) in a Bioactivity: Triamterene D5 is deuterium labeled Triamterene, which can voltage-dependent manner, which used as a mild diuretic. block epithelial Na+ channel (ENaC) in a voltage-dependent manner, which used as a mild diuretic.

Purity: 99.17% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg 100 mg, 500 mg

Trichlormethiazide Vinpocetine Cat. No.: HY-B0235 (Ethyl apovincaminate) Cat. No.: HY-13295

Bioactivity: is a thiazide diuretic with properties Bioactivity: Vinpocetine(Cavinton; Ethyl apovincaminate) is a selective for similar to those of . PDE1 (IC50 = 21 μM). Also blocks voltage-gated Na+ channels. IC50 value: Target: PDE1; Na+ channel

Purity: 98.67% Purity: 99.82% 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, 200 mg, 500 mg

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XEN907 YM758 Cat. No.: HY-19958 Cat. No.: HY-U00309

Bioactivity: XEN907 is a novel spirooxindole NaV1.7 blocker, inhibits Bioactivity: YM758 is a “funny” I f current channel ( If channel) hNaV1.7 with IC50 of 3 nM. inhibitor.

Purity: 99.55% 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

Zonisamide Zonisamide sodium (AD 810; CI 912) Cat. No.: HY-B0124 (AD 810 sodium; CI 912 sodium) Cat. No.: HY-B0124A

Bioactivity: Zonisamide is a 1,2 benzisoxazole derivative and the first Bioactivity: Zonisamide sodium is a 1,2 benzisoxazole derivative and the agent of this chemical class to be developed as an first agent of this chemical class to be developed as an antiepileptic drug. antiepileptic drug.

Purity: 99.72% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 200 mg, 500 mg 200 mg, 500 mg

118 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] TRP Channel Transient receptor potential channels

TRP Channel (Transient receptor potential channel) is a group of ion channels located mostly on the plasma membrane of numerous human and animal cell types. There are about 28 TRP channels that share some structural similarity to each other. These are grouped into two broad groups: Group 1 includes TRPC ("C" for canonical), TRPV ("V" for vanilloid), TRPM ("M" for melastatin), TRPN, and TRPA. In group 2, there are TRPP ("P" for polycystic) and TRPML ("ML" for mucolipin). Many of these channels mediate a variety of sensations like the sensations of pain, hotness, warmth or coldness, different kinds of tastes, pressure, and vision. TRP channels are relatively non-selectively permeable to cations, including sodium, calcium and magnesium. TRP channels are initially discovered in trp-mutant strain of the fruit fly Drosophila. Later, TRP channels are found in vertebrates where they are ubiquitously expressed in many cell types and tissues. TRP channels are important for human health as mutations in at least four TRP channels underlie disease.

www.MedChemExpress.com 119 TRP Channel Inhibitors & Modulators

(-)- (Z)- Cat. No.: HY-75161 (; Civamide; cis-Capsaicin) Cat. No.: HY-B1583

Bioactivity: (-)-Menthol is a key component of peppermint oil that binds Bioactivity: (Z)-Capsaicin is the cis isomer of capsaicin, acts as an and activates transient receptor potential melastatin 8 ( orally active TRPV1 agonist, and is used in the research of TRPM8), a Ca 2+-permeable nonselective cation channel, neuropathic pain. 2+ [1] [1] to increase [Ca ] i . Antitumor activity . Purity: 98.0% Purity: 99.96% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g 10 mg, 50 mg

A-1165442 A-967079 Cat. No.: HY-12428 Cat. No.: HY-108463

Bioactivity: A-1165442 is a potent, competitive and orally available TRPV1 Bioactivity: A-967079 is a selective TRPA1 receptor antagonist with IC50s antagonist with an IC of 9 nM for human TRPV1. 50 of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and has good penetration into the CNS.

Purity: 99.49% Purity: 98.66% 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 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

ABT-239 AM-0902 Cat. No.: HY-12195 Cat. No.: HY-108329

Bioactivity: ABT-239 is a novel, highly efficacious, Bioactivity: AM-0902 is a potent, selective transient receptor potential A1

non- class of H3R antagonist and a transient ( TRPA1) antagonist with IC50s of 71 and 131 nM for rTRPA1 receptor potential vanilloid type 1 ( TRPV1) and hTRPA1, respectively. antagonist.

Purity: 98.94% Purity: 99.39% 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 5 mg, 10 mg, 50 mg, 100 mg

AMG 333 AMG 517 Cat. No.: HY-112703 Cat. No.: HY-10634

Bioactivity: AMG 333 is a potent and highly selective TRPM8 antagonist Bioactivity: AMG 517 is a potent and selective vanilloid receptor-1 ( TRPV1) antagonist with an IC of 0.5 nM. with an IC50 of 13 nM. 50

Purity: >98% Purity: 99.87% 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

AMG2850 AMG9810 Cat. No.: HY-104059 Cat. No.: HY-101736

Bioactivity: AMG2850 is a potent, orally bioavailable and selective Bioactivity: AMG9810 is a selective and competitive vanilloid receptor 1 (

transient receptor potential melastatin 8 (TRPM8) antagonist TRPV1) antagonist with IC50 values of 24.5 and 85.6 nM for [1] . human and rat TRPV1, repectively.

Purity: >98% Purity: 99.42% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

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

Asivatrep BCTC (PAC-14028) Cat. No.: HY-12777 Cat. No.: HY-19960

Bioactivity: Asivatrep (PAC-14028) is a potent and selective transient Bioactivity: BCTC is a potent and specific inhibitor of transient receptor receptor potential vanilloid type I ( TRPV1) antagonist. potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.

Purity: 95.03% Purity: 97.23% Clinical Data: Phase 3 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

BI-749327 Caffeic acid Cat. No.: HY-111925 Cat. No.: HY-N0172

Bioactivity: BI-749327 is an orally bioavailable TRPC6 antagonist with an Bioactivity: Caffeic acid is an inhibitor of both TRPV1 ion channel and [1] 5-Lipoxygenase ( 5-LO). IC50 of 13 nM in mice .

Purity: >98% Purity: 98.80% Clinical Data: No Development Reported Clinical Data: Phase 4 Size: 500 mg, 250 mg Size: 10mM x 1mL in DMSO, 100 mg, 5 g

Camphor Capsaicin ((±)-) Cat. No.: HY-N0808 ((E)-Capsaicin; 8-Methyl-N-vanillyl-trans-6-nonenamide) Cat. No.: HY-10448

Bioactivity: Camphor ((±)-Camphor) is a topical anti-infective and Bioactivity: Capsaicin is a TRPV1 agonist with an EC50 of 0.29 μM in anti-pruritic and internally as a stimulant and carminative. HEK293 cells. However, Camphor is poisonous when ingested. Antiviral, antitussive, and anticancer activities [1]. Camphor i…

Purity: 98.0% Purity: 98.39% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 50 mg, 100 mg

Capsazepine Cardamonin Cat. No.: HY-15640 (Alpinetin chalcone; Cardamomin) Cat. No.: HY-N1378

Bioactivity: is a synthetic analogue of the sensory neurone Bioactivity: Cardamonin is a novel antagonist of hTRPA1 cation channel excitotoxin, and an antagonist of TRPV1 receptor with an with an IC50 of 454 nM. IC50 of 562 nM.

Purity: 99.0% 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, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Chembridge-5861528 D-3263 (TCS 5861528) Cat. No.: HY-15065 Cat. No.: HY-16162

Bioactivity: Chembridge-5861528 is a TRPA1 channel blocker that antagonizes Bioactivity: D-3263 is an agonist of transient receptor potential AITC- and 4-HNE-evoked calcium influx (IC50 values are 14.3 melastatin member 8 ( TRPM8) with potential antineoplastic and 18.7μM respectively). activity.

Purity: 97.04% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 1 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 121

D-3263 hydrochloride Diphenyleneiodonium chloride Cat. No.: HY-16162A (DPI) Cat. No.: HY-100965

Bioactivity: D-3263 hydrochloride is an enteric-coated, orally bioavailable Bioactivity: Diphenyleneiodonium chloride is a NADPH oxidase ( NOX) (transient receptor potential melastatin member 8) TRPM8 inhibitor and also functions as a TRPA1 activator with an agonist. EC50 of 1 to 3 μM.

Purity: 98.86% Purity: 99.87% Clinical Data: Phase 1 Clinical Data: Phase 4 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

DS88790512 EIPA Cat. No.: HY-112298 (L593754; MH 12-43; Ethylisopropylamiloride) Cat. No.: HY-101840

Bioactivity: DS88790512 is a potent, selective, and orally bioavailable Bioactivity: EIPA is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. TRPC6 inhibitor with an IC of 11 nM. 50 EIPA also inhibits Na+/H+-exchanger ( NHE) and macropinocytosis.

Purity: >98% Purity: 99.73% 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

EIPA hydrochloride (L593754 hydrochloride; MH 12-43 GSK1016790A hydrochloride; Ethylisopropylamiloride hydrochloride) Cat. No.: HY-101840A Cat. No.: HY-19608

Bioactivity: EIPA hydrochloride (L593754 hydrochloride) is a TRPP3 channel Bioactivity: GSK1016790A is a potent transient receptor potential vanilloid [1] 4 ( TRPV4) activator. inhibitor with an IC50 of 10.5 μM . EIPA also inhibits Na+/H+-exchanger ( NHE) [2] and macropinocytosis [3].

Purity: >98% Purity: 97.62% 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 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

GSK2193874 GSK3395879 Cat. No.: HY-100720 Cat. No.: HY-112202

Bioactivity: GSK2193874 is an orally active, potent, and selective TRPV4 Bioactivity: GSK3395879 is a selective and orally bioavailable transient receptor potential vanilloid-4 ( TRPV4) antagonist with an antagonist with IC50 of 2 nM and 40 nM for rTRPV4 and [1] hTRPV4. IC50 of 1 nM for hTRPV4 .

Purity: 99.18% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 100 mg, 250 mg, 500 mg 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

HC-030031 HC-067047 Cat. No.: HY-15064 Cat. No.: HY-100208

Bioactivity: HC-030031 is a potent and selective TRPA1 inhibitor, which Bioactivity: HC-067047 is a potent and selective TRPV4 antagonist with

antagonizes AITC- and formalin-evoked calcium influx with IC50s of 48 nM, 133 nM, and 17 nM for human, rat, and mouse IC s of 6.2±0.2 and 5.3±0.2 μM, respectively. 50 TRPV4.

Purity: 98.01% Purity: 99.95% 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, 10 mg, 25 mg, 50 mg, 100 mg

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

HC-070 Cat. No.: HY-112302 (AG-3-5) Cat. No.: HY-11062

Bioactivity: HC-070 is an antagonist of TRPC4/TRPC5, with IC50s of 9.3 nM Bioactivity: Icilin(AG 3-5) is a synthetic super-agonist of TRPM8 ion and 46 nM for hTRPC5 and hTRPC4 in cells, respectively. channel.

Purity: 98.23% Purity: 96.0% 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, 50 mg

Imperatorin JNJ-17203212 (Ammidin) Cat. No.: HY-N0285 Cat. No.: HY-100129

Bioactivity: Imperatorin is an effective of NO synthesis inhibitor ( Bioactivity: JNJ-17203212 is a novel and selective TRPV1 antagonist, with IC50 of 65 nM and 102 nM for human TRPV1 and rat TRPV1. IC50=9.2 μmol), which also is a BChE inhibitor ( IC50=31.4

μmol). Imperatorin is a weak agonist of TRPV1 with EC50 of 12.6±3.2 μM. Purity: 98.11% 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, 25 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

JT010 JYL 1421 Cat. No.: HY-111132 (SC 0030) Cat. No.: HY-100668

Bioactivity: JT010 is a potent agonist of TRPA1 with an EC50 of 0.65 nM. Bioactivity: JYL 1421 is a TRPV1 receptor antagonist, with an IC50 of 8 nM.

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

Mavatrep Mifamurtide (CGP-19835; MTP-PE; MTP-cephalin; CGP19835; (JNJ-39439335) Cat. No.: HY-16935 L-MTP-PE; MLV19835) Cat. No.: HY-13682

Bioactivity: Mavatrep is an orally bioavailable TRPV1 antagonist (Ki=6.5 Bioactivity: Mifamurtide(CGP19835; MTP-PE) is a drug against osteosarcoma. nM), exhibits minimal effect on the enzymatic activity (IC50 > 25 μM) of CYP isoforms 3A4, 1A2, and 2D6.

Purity: 99.79% Purity: 99.0% Clinical Data: Phase 1 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

ML204 ML204 hydrochloride Cat. No.: HY-12949 Cat. No.: HY-12949A

Bioactivity: ML204 is a novel potent antagonist that selectively modulates Bioactivity: ML204 hydrochloride is a novel, potent, selective TRPC4 native TRPC4/C5 ion channels. channel inhibitor with IC50 of 0.96 uM. exhibit 19-fold selectivity against TRPC6 channels in similar fluorescent assays. target: ML204 IC50: 0.96 uM In vitro: ML204 inhibited TRPC4β-mediated intracellular Ca2+ rise. ML204 at 10 μm showed… Purity: 98.31% Purity: 99.37% 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, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

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N-(p-amylcinnamoyl) Anthranilic Acid (Pseudocapsaicin; Pelargonic acid vanillylamide; (ACA) Cat. No.: HY-118628 Nonanoic acid vanillylamide) Cat. No.: HY-17568

Bioactivity: N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is a broad spectrum Bioactivity: Nonivamide is a

Phospholipase A2 (PLA2) inhibitor and TRP channel blocker EC50 value of 5.1 mg/L in static tests. [1] [2]. N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is also an effective reversible inhibitor of calcium-activa… Purity: 98.81% Purity: 98.15% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 25 mg, 50 mg, 100 mg 100 mg, 500 mg, 5 g

Optovin PF-4840154 Cat. No.: HY-12809 Cat. No.: HY-18779

Bioactivity: Optovin is a reversible photoactive TRPA1 activator; Bioactivity: PF-4840154 is a potent, selective agonist of the rat and human

stimulates human TRPA1 channels in vitro and enables repeated TrpA1 channel with EC50s of 97 and 23 nM, respectively. photoactivation of motor behaviors in wild-type zebrafish (EC50 = 2 μM).

Purity: 99.54% Purity: 99.96% 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

Pico145 Podocarpic acid (HC-608) Cat. No.: HY-101507 Cat. No.: HY-N2318

Bioactivity: Pico145 is a remarkable inhibitor of TRPC1/4/5 channels, Bioactivity: Podocarpic acid is a natural product, which has the best inhibits (−)-englerin A-activated TRPC4/TRPC5 channels, with all-round positive effect and acts as a novel TRPA1

IC50s of 0.349 and 1.3 nM in cells, and shows no effect on activator. TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.

Purity: 99.42% Purity: 99.37% 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

Probenecid Pyr10 Cat. No.: HY-B0545 Cat. No.: HY-19408

Bioactivity: Probenecid is a potent and selective agonist of transient Bioactivity: Pyr10is a novel TRPC3-selective inhibitor, IC50 of Ca2+ influx receptor potential vanilloid 2 ( TRPV2) channels. Probenecid inhibition by Pyr10 in carbachol-stimulated also inhibits pannexin 1 channels. YFP-TRPC3-transfected HEK293 cells for ROCE and thapsigargin-depleted native RBL-2H3 cells for SOCE is 0.72 uM and 13.08 uM. Purity: 99.91% Purity: 99.60% 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, 50 mg

Pyr3 Pyr6 Cat. No.: HY-108465 Cat. No.: HY-12504

Bioactivity: Pyr3 is a selective inhibitor of transient receptor potential Bioactivity: Pyr6 is a selective inhibitor of TRPC3 with IC50 of 0.49

canonical channel 3 (TRPC3), with an IC50 of 700 nM for uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells). IC50 value: 0.49 uM [1] Target: TRPC3 TRPC3-mediated Ca 2+ influx. inhibitor Pyr6 is a selective SOCE inhibitor (Yonetoku et al., 2008; Sweeney et al., 2009), Pyr6 displayed 37-fold (1.58 OM)… Purity: 99.89% Purity: 99.42% 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 5 mg, 10 mg

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

RN-1734 RN-1747 Cat. No.: HY-19975 Cat. No.: HY-19976

Bioactivity: RN-1734 is selective antagonist of the TRPV4 channel, Bioactivity: RN-1747 is a selective transient receptor potential cation

completely antagonizes 4αPDD-mediated activation of TRPV4 with channel subfamily V member 4 (TRPV4) agonist, with EC50 comparable, low micromolar IC s for all three species 50 values are 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and (hTRPV4: 2.3 μM, mTRPV4: 5.9 μM, rTRPV4: 3.2 μM) [1]. RN-1… rTRPV4 respectively. RN-1747 also antagonizes TRPM8, with… Purity: 99.01% 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

Rosiglitazone Rosiglitazone maleate (BRL49653) Cat. No.: HY-17386 (BRL 49653C) Cat. No.: HY-14600

Bioactivity: Rosiglitazone (BRL49653) is a selective PPARγ agonist with Bioactivity: Rosiglitazone maleate is a potent and selective activator of PPARγ, with EC s of 30 nM, 100 nM and 60 nM for PPARγ1, EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and 50

PPARγ, respectively. PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of … Purity: 99.21% Purity: 99.25% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg, 500 mg 50 mg, 200 mg

RQ-00203078 SAR7334 Cat. No.: HY-18662 Cat. No.: HY-15699

Bioactivity: RQ-00203078 is a highly selective, potent and orally available Bioactivity: SAR7334 is a potent TRPC6 (Transient receptor potential TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and cation channel, subfamily C, member 6) inhibitor. human channels respectively), exhibits >350-fold selectivity for TRPM8 over TRPV4, TRPV1 and TRPA1.

Purity: 99.35% Purity: 99.91% 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, 50 mg, 100 mg

SAR7334 hydrochloride SB-366791 Cat. No.: HY-15699A Cat. No.: HY-12245

Bioactivity: SAR7334 hydrochloride is a potent and specific TRPC6 Bioactivity: SB-366791 is a potent , competitive and selective vanilloid receptor (VR1/TRPV1) antagonist with IC50 of 5.7±1.2 nM inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM. target: VR1/TRPV1 IC 50: 5.7±1.2 nM [1] SB-366791 produced a concentration-dependent inhibition of the response to capsaicin with an apparent pKb of 7.74±0.08. Schild analysis… Purity: 95.30% Purity: 98.64% 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

SB-705498 SKF-96365 hydrochloride Cat. No.: HY-10633 Cat. No.: HY-100001

Bioactivity: SB-705498 is a potent, selective and orally bioavailable Bioactivity: SKF-96365 hydrochloride is a non-selective TRP Channel transient receptor potential vanilloid 1 (TRPV1) receptor blocker.

antagonist with a pIC50 of 7.1.

Purity: 99.61% Purity: 99.44% 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, 200 mg

www.MedChemExpress.com 125

SN 2 TC-I 2014 Cat. No.: HY-16696 Cat. No.: HY-110199

Bioactivity: SN 2 is a novel and potent activator of TRPML3 ion channel Bioactivity: TC-I 2014 (compound 5) is a potent -containing transient receptor potential melastatin 8 (TRPM8) with EC50 of 1.8±0.13 μM. antagonist, with IC50 values of 0.8 nM, 3.0 nM and 4.4 nM for canine, human and rat channels respectively. TC-I 2…

Purity: 99.99% 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, 10 mg, 50 mg 5 mg

TRPA1 Antagonist 1 TRPC6-IN-1 Cat. No.: HY-111494 Cat. No.: HY-101547

Bioactivity: TRPA1 Antagonist 1 is a methylene phosphate prodrug which Bioactivity: TRPC6-IN-1 is a Transient Receptor Potential Canonical 6

converts to its active parent drug, a TRPA1 antagonist with Channel (TRPC6) inhibitor, with an EC50 of 4.66 μM. an IC50 of 8 nM.

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

TRPM8 antagonist 2 TRPM8 antagonist WS-3 Cat. No.: HY-112430 Cat. No.: HY-W014325

Bioactivity: TRPM8 antagonist 2 is a potent and selective TRPM8 Bioactivity: TRPM8 antagonist WS-3 is an agonist of TRPM8 with an EC50 antagonist, with an IC of 0.2 nM, used in the research of 50 of 3.7 μM. neuropathic pain syndromes.

Purity: 98.20% Purity: 99.21% 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 g

TRPV antagonist 1 TRPV4 agonist-1 Cat. No.: HY-U00330 Cat. No.: HY-114400

Bioactivity: TRPV antagonist 1 is a transient receptor potential vanilloid Bioactivity: TRPV4 agonist-1 is a transient receptor potential vanilloid 4 (TRPV) antagonist, with an IC of < 250 nM. 2+ 50 (TRPV4) agonist with an EC 50 of 60 nM in the hTRPV4 Ca assay [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: 100 mg, 250 mg, 500 mg

WS-12 Cat. No.: HY-108449

Bioactivity: WS-12 is an agonist of TRPM8 with an EC50 of 39 nM.

Purity: 99.03% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 5 mg, 10 mg

126 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] URAT1 Urate transporter 1;SLC22A12

URAT1, a member of the OAT (organic anion transporter) family was first cloned from the human kidney, where it is localized to the apical (brush border) membrane of renal proximal tubular cells. URAT1 mediates the reabsorption of uric acid, thereby regulating blood uric acid concentrations. Impairment in URAT1 activity, either due to polymorphisms, or drug-drug interactions, can have toxicological consequences. In the kidney, URAT1 is distributed along the renal tubular cell membrane and involved in reabsorption and excretion of uric acid, organic acids, drugs and their metabolites. Uric acid is taken up by OAT1 and OAT3 from the blood and reabsorbed into renal tubular cells via URAT1, in exchange for dicarboxylic acid. URAT1, along with OAT4 mediates uptake of uric acid from the renal tubule into renal tubular cells in exchange for organic anions such as lactic acid and nicotinic acid. This exchange is electroneutral and can be trans-stimulated by Cl - gradients and gradients of lactate transported by the sodium-monocarboxylate transporter. In the salivary glands, URAT1 is distributed along the entire surface, including the ductal and acinar cells, suggesting a role in the transport of organic acids and uric acid in the whole salivary gland.

www.MedChemExpress.com 127 URAT1 Inhibitors & Modulators

Lesinurad Lesinurad sodium (RDEA594) Cat. No.: HY-15258 (RDEA-594 sodium) Cat. No.: HY-15258A

Bioactivity: Lesinurad is a URAT1 and OAT inhibitor, is determined to be Bioactivity: Lesinurad sodium is a URAT1 and OAT inhibitor, is determined a substrate for the kidney transporters OAT1 and OAT3 with to be a substrate for the kidney transporters OAT1 and OAT3

Km values of 0.85 and 2 µM, respectively. with Km values of 0.85 and 2 µM, respectively.

Purity: 99.96% Purity: 99.92% 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, 200 mg

URAT1 inhibitor 1 Verinurad Cat. No.: HY-114309 (RDEA3170) Cat. No.: HY-16733

Bioactivity: URAT1 inhibitor 1 (1g) is a uric acid transporter 1 (URAT1) Bioactivity: Verinurad (RDEA3170) is a highly potent and specific URAT1 inhibitor, with an IC of 32 nM. URAT1 inhibitor 1 has [1] 50 inhibitor with an IC50 of 25 nM . potential to treat hyperuricemia associated with gout [1].

Purity: >98% Purity: 98.0% 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

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