A-317491

SKU: orb1296280

Description

A-317491 (ABT 202) is a potent, non-nucleotide antagonist of P2X3 (Ki: 22 nM) and P2X2/3 (Ki: 9 nM) receptors, effectively inhibiting receptor-mediated calcium flux. This compound is widely used in vitro and in vivo to investigate purinergic signaling in pain, cough, and inflammatory pathways.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 475205-49-3
• MW: 565.57
• Purity: 98.08%
• Formula: C₃₃H₂₇NO₈
• SMILES: OC(=O)c1cc(C(O)=O)c(cc1C(O)=O)C(=O)N(Cc1cccc(Oc2ccccc2)c1)[C@H]1CCCc2ccccc12
• Target: P2X Receptor
• Solubility: Ethanol:90 mg/mL (159.13 mM);DMSO:47 mg/mL (83.1 mM);H2O:< 0.1 mg/mL (insoluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.54 mM)

Bioactivity

• Target IC50:
  P2X3:22 nM(Ki, cell free)|P2X2:9 nM (Ki, cell free)
• In Vivo:
  A-317491 dose-dependently reduces complete Freund's adjuvant-induced thermal hyperalgesia in the rat (ED50: 30 μM L/kg s.c.). A-317491 is most potent in attenuating both thermal hyperalgesia and Mechanical allodynia after chronic nerve constriction injury (ED50: 10-15 μM L/kg s.c.). Although active in chronic pain models, A-317491 is i effective in reducing nociception in animal models of acute pain, postoperative pain, and visceral pain (ED50 >100 μM L/kg s.c.). A-317491 is effective in reducing pain associated behavior in several animal models of inflammatory and neuropathic pain when administered systemically.
• In Vitro:
  A-317491 blocks recombinant human and rat P2X3 and P2X2/3 receptor-mediated calcium flux (Ki = 22-92 nM) and is highly Selective IC50 >10 μM) over Other P2 receptors and Other ion channels, neurotransmitter receptors, and enzymes.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

ABT202, ABT-202, ABT 202, A 317491, A317491, A-317491, calcium, inhibit, inflammatory, neuropathic, pain, Inhibitor, Human P2X3, flux, P2X Receptor, P2X2, P2X2/3, P2X3, P2XRs, P2XReceptor

Compound Identifiers

PubChem CID

9829395