PEAQX tetrasodium hydrate (459836-30-7 free base)

SKU: orb1706833

Description

PEAQX tetrasodium hydrate (CAS 459836-30-7 free base) is a potent, selective, and orally bioavailable NMDA receptor antagonist. It demonstrates high selectivity for GluN2A-containing receptors (IC50 270 nM, hNMDAR 1A/2A) over GluN2B subtypes. This compound is a valuable research tool for investigating NMDA receptor function in neurological disease models, both in vitro and in vivo.

Research Area

Cell Biology, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• MW: 560.15
• Purity: 99.00% (May vary between batches)
• Formula: C₁₇H₁₅BrN₃Na₄O₆P
• SMILES: [O-]P([O-])(C(C1=CC=CC2=C1N=C(C([O-])=N2)[O-])N[C@H](C3=CC=C(C=C3)Br)C)=O.[H]O[H].[Na+].[Na+].[Na+].[Na+]
• Target: Apoptosis,iGluR,NMDAR
• Solubility: H2O:22.9 mg/mL (40.88 mM)

Bioactivity

• Target IC50:
  NMDAR 1A/2A (human):270 nM|NMDAR 1A/2B (human):29600 nM
• 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 . 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.
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• 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).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PEAQX tetrasodium Hydrate, PEAQX tetrasodium hydrate, PEAQX tetrasodium hydrate (459836-30-7 free base), Apoptosis, 459836-30-7, 459836-30-7 free base, iGluR, NVP-AAM077 tetrasodium hydrate, NVP-AAM077 tetrasodium Hydrate, NMDA

Compound Identifiers

PubChem CID

71311756