A 317491 sodium salt

Key Product Details

Product Description

A 317491 sodium salt is a selective, high affinity non-nucleotide P2X₃ and P2X_2/3 receptor antagonist (K_i values are 9, 22, 22 and 92 nM at human P2X_2/3, rat P2X₃, human P2X₃ and rat P2X_2/3, respectively); blocks recombinant human and rat P2X₃ and P2X_2/3 receptor-mediated calcium flux (K_i = 22 - 92 nM). Exhibits selectivity over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes (IC₅₀ > 5 μM). Reduces mechanical allodynia and thermal hyperalgesia in the CCI in vivo models. Antinociceptive.

Product Specifications for A 317491 sodium salt

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for A 317491 sodium salt

The following data is based on the product molecular weight 609.54.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.64 mL	8.20 mL	16.41 mL
5 mM	0.33 mL	1.64 mL	3.28 mL
10 mM	0.16 mL	0.82 mL	1.64 mL
50 mM	0.03 mL	0.16 mL	0.33 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Neelands 2', 3'-O-(2,4,6,trinitrophenyl)-ATP and A-317491 are competitive antagonists at a slowly desensitizing chimeric human P2X₃ receptor. Br.J.Pharmacol. 2003 PMID: 12967950
• Mansoor X-ray structures define human P2X₃ receptor gating cycle and antagonist action. Nature 2016 PMID: 27626375
• McGaraughty Effects of A-317491, a novel and selective P2X₃/P2X_2/3 receptor antagonist, on neuropathic, inflammatory and chemogenic nociception following intrathecal and intraplantar administration. Br.J.Pharmacol. 2003 PMID: 14623769
• McGaraughty Endogenous opioid mechanisms partially mediate P2X3/P2X2/3-related antinociception in rat models of inflammatory and chemogenic pain but not neuropathic pain. Br.J.Pharmacol. 2005 PMID: 16041397
• Jarvis A-317491, a novel potent and selective non-nucleotide antagonist of P2X₃ and P2X_2/3 receptors, reduces chronic inflammatory and neuropathic pain in the rat. Proc.Nat.Acad.Sci.USA 2002 PMID: 12482951

Product Documents for A 317491 sodium salt