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Home , Ampakine, Apimostinel, Fanapanel, Farampator, Mephenesin, PEAQX

iGluR Ionotropic glutamate receptors

iGluR (ionotropic ) is a -gated channel that is activated by the glutamate. iGluR are integral membrane 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 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 . influx through NMDA receptors leads to persistent modifications in the strength of synaptic transmission.

www.MedChemExpress.com 1 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 .

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 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 : The (S)- but not [1] [2]. (R)- 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 (Naproxen 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 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- 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 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

2 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 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] and mild cognitive impairment (MCI). (pIC 50=5) . Purity: >98% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 500 mg, 100 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 nootropics and neuroprotective Bioactivity: Apimostinel is an oral NMDA receptor . 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 -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 opioid neuropeptide, Bioactivity: Dynorphin A (1-10) an endogenous opioid neuropeptide, binds to binds to extracellular loop 2 of the κ-opioid receptor. extracellular loop 2 of the κ-opioid receptor. Dynorphin A

Dynorphin A (1-10) (TFA) also blocks NMDA-activated current (1-10) also blocks NMDA-activated current with an IC50 of with an IC of 42.0 μM. 50 42.0 μM.

Purity: 95.04% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg

Eliprodil (SL-820715) Cat. No.: HY-12881 (ZK200775; MPQX) Cat. No.: HY-15069

Bioactivity: (SL-820715) is a non-competitive NR2B-NMDA receptor Bioactivity: Fanapanel (ZK200775) is a highly selective AMPA/kainate antagonist(IC50=1 uM), less potent for NR2A- and antagonist with little activity against NMDA; have Ki values NR2C-containing receptors(IC50> 100 uM). of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.

Purity: 99.67% Purity: 99.93% Clinical Data: Phase 2 Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 10 mg, 50 mg

4 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 whose Bioactivity: Felbamate (hydrate) (W-554 (hydrate)) is a potent nonsedative clinical effect may be related to the inhibition of anticonvulsant whose clinical effect may be related to the N-methyl-D-aspartate (NMDA). inhibition of N-methyl-D-aspartate (NMDA) .

Purity: 98.30% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 10 mg, 50 mg, 100 mg, 200 mg

Flupirtine Maleate (D 9998) Cat. No.: HY-17001A Cat. No.: HY-17001

Bioactivity: Flupirtine(D 9998) is a selective neuronal potassium channel Bioactivity: Flupirtine Maleate(D 9998) is a selective neuronal potassium opener that also has NMDA receptor antagonist properties. that also has NMDA receptor antagonist properties. IC50 Value: Target: Potassium channel; NMDA receptor in vitro: High concentrations of flupirtine antagonized inward currents to NMDA(200 microM) at -70 mV with… Purity: >98% Purity: 99.97% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg, 100 mg, 500 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg, 500 mg gamma-DGG Glycine (γDGG; γ-D-Glutamylglycine) Cat. No.: HY-100785 Cat. No.: HY-Y0966

Bioactivity: gamma-DGG is a competitive AMPA receptor blocker. Bioactivity: Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.

Purity: 98.08% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 g

GNE 0723 GNE 5729 Cat. No.: HY-108337 Cat. No.: HY-107409

Bioactivity: GNE 0723 is a brain permeable positive allosteric modulator of Bioactivity: GNE 5729 is a brain permeable positive allosteric modulator of

NMDAR, with an EC50 of 21 nM for GluN2A, 7.4 and 6.2 μM NMDAR, with an EC50 of 37 nM for GluN2A, 4.7 and 9.5 μM for GluN2C and GluN2D, respectively. for GluN2C and GluN2D, respectively.

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

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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 -dependent AMPAR/γ-8 receptor occupancy in mouse , 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 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 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

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

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

Bioactivity: Linalool is natural monoterpene in essential olis of Bioactivity: LY450108 is an coriander, acts as a competitive antagonist of Nmethyl alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid d-aspartate (NMDA) receptor, with anti-tumor, (AMPA) receptor potentiator. IC50 value: Target: AMPA anti-cardiotoxicity activity [1]. receptors mediate most of the excitatory 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 .

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 . 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 strychnine-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-adrenergic receptor.

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

NT 13 Omberacetam (TPPT) Cat. No.: HY-P7060 (GVS-111; SGS-111) Cat. No.: HY-17456

Bioactivity: NT 13 (TPPT) is a having the sequence Bioactivity: Omberacetam (GVS-111) is a promoted and prescribed L-threonyl-L-prolyl-L-prolyl-L-threonine amide. NT 13 is a in Russia and neighbouring countries as a nootropic. partial N-methyl-D-aspartate receptor ( NMDAR) agonist used in the study of depression, , 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 .

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

8 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- 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 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

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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 with an IC50 of 10 [1] nM. .

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

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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

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