A 317491 sodium salt

Name: A 317491 sodium salt
Brand: Tocris Bioscience
SKU: 6493

Tocris Bioscience, part of Bio-Techne | Catalog # 6493

COA / SDS

Selective, high affinity P2X3 and P2X2/3 antagonist; antinociceptive

Key Product Details

Description:	Selective, high affinity P2X₃ and P2X_2/3 antagonist; antinociceptive
Chemical Name:	5-[[[(3-Phenoxyphenyl)methyl][(1S)-1,2,3,4-tetrahydro-1-naphthalenyl]amino]carbonyl]-1,2,4-benzenetricarboxylic acid disodium salt
Purity:	≥98% (HPLC)
Molecular Weight:	609.54

View Full Technical Details for A 317491 sodium salt

Technical Data
Citations

Biological Activity for A 317491 sodium salt

A 317491 sodium salt is a selective, high affinity non-nucleotide P2X₃ and P2X_2/3 receptor antagonist (K_ivalues 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.

Compound Libraries for A 317491 sodium salt

A 317491 sodium salt is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for A 317491 sodium salt

M. Wt	609.54
Formula	C₃₃H₂₅NO₈Na₂
Storage	Store at -20°C
Purity	≥98% (HPLC)
Smiles	O=C(C1=CC(C(O)=O)=C(C(N([C@H]2CCCC3=CC=CC=C23)CC4=CC(OC5=CC=CC=C5)=CC=C4)=O)C=C1C(O[Na])=O)O[Na]

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

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for A 317491 sodium salt

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	60.95	100

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for A 317491 sodium salt

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