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PEAQX tetrasodium hydrate

Catalog No. T16451   CAS T16451
Synonyms: NVP-AAM077 tetrasodium hydrate, PEAQX tetrasodium hydrate (459836-30-7 free base), PEAQX tetrasodium hydrate

PEAQX tetrasodium hydrate (PEAQX tetrasodium hydrate (459836-30-7 free base)) is an orally available NMDA antagonist that is potent and selective. The IC50 value of PEAQX tetrasodium hydrate (459836-30-7 free base) against hNMDAR 1A/2A was 270 nM and 29600 nM against hNMDAR 1A/2B, respectively.

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PEAQX tetrasodium hydrate Chemical Structure
PEAQX tetrasodium hydrate, CAS T16451
Pack Size Availability Price/USD Quantity
1 mg In stock $ 71.00
5 mg In stock $ 167.00
10 mg In stock $ 250.00
25 mg In stock $ 430.00
50 mg In stock $ 636.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PEAQX tetrasodium hydrate (PEAQX tetrasodium hydrate (459836-30-7 free base)) is an orally available NMDA antagonist that is potent and selective. The IC50 value of PEAQX tetrasodium hydrate (459836-30-7 free base) against hNMDAR 1A/2A was 270 nM and 29600 nM against hNMDAR 1A/2B, respectively.
Targets&IC50 NMDAR 1A/2B (human):29600 nM, NMDAR 1A/2A (human):270 nM
In vitro PEAQX has a high binding affinity for NMDA receptors (IC50=8 nM), and a functional preference in excess of 100-fold for hNMDA 1A/2A (IC50=of 270 nM) over 1A/2B receptors (IC50=29,600 nM).[1]
In vivo PEAQX is practically inactive in Xenopus oocytes expressing hNMDA 1A/2B receptors, displays an ED50 value of 23 mg/kg in the MES test [1].
Sprague-Dawley rats were treated on PN7, PN9, and PN11 with PCP (10 mg/kg), PEAQX (NR2A-preferring antagonist; 10, 20, or 40 mg/kg), or ifenprodil (selective NR2B antagonist; 1, 5, or 10 mg/kg) and sacrificed for measurement of caspase-3 activity (an index of apoptosis) or allowed to age and tested for locomotor sensitization to PCP challenge on PN28-PN35. PCP or PEAQX on PN7, PN9, and PN11 markedly elevated caspase-3 activity in the cortex; ifenprodil showed no effect. Striatal apoptosis was evident only after subchronic treatment with a high dose of PEAQX (20 mg/kg). Animals treated with PCP or PEAQX on PN7, PN9, and PN11 showed a sensitized locomotor response to the PCP challenge on PN28-PN35.[2]
Synonyms NVP-AAM077 tetrasodium hydrate, PEAQX tetrasodium hydrate (459836-30-7 free base), PEAQX tetrasodium hydrate
Molecular Weight 560.15
Formula C17H15BrN3Na4O6P
CAS No. T16451

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 22.9 mg/mL (41.0 mM), Sonication and heating are recommended.

TargetMolReferences and Literature

1. Auberson YP, et al. 5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonists with a preference for the human 1A/2A, rather than 1A/2B receptor composition. Bioorg Med Chem Lett. 2002;12(7):1099-1102. 2. Anastasio NC, et al. Differential role of N-methyl-D-aspartate receptor subunits 2A and 2B in mediating phencyclidine-induced perinatal neuronal apoptosis and behavioral deficits. Neuroscience. 2009;163(4):1181-1191. 3. Yu X, Jia L, et al. Src is Implicated in Hepatic Ischemia Reperfusion-Induced Hippocampus Injury and Long-Term Cognitive Impairment in Young Mice via NMDA Receptor Subunit 2A Activation. Neuroscience. 2018;391:1-12.

Related compound libraries

This product is contained In the following compound libraries:
Membrane Protein-targeted Compound Library Anti-Neurodegenerative Disease Compound Library Neuronal Signaling Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

PEAQX tetrasodium hydrate T16451 Apoptosis Membrane transporter/Ion channel Neuroscience NMDAR iGluR NVP-AAM077 tetrasodium hydrate PEAQX tetrasodium hydrate (459836-30-7 free base) 459836-30-7 free base 459836-30-7 NVP-AAM077 tetrasodium Hydrate PEAQX tetrasodium Hydrate inhibitor inhibit

 

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