A-317491

A-317491 is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux[1][2].

Product Specifications

CAS Number

[475205-49-3]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

P2X Receptor

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Cancer-programmed cell death

Field of Research

Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/A-317491.html

Purity

98.64

Solubility

DMSO : ≥ 47 mg/mL

Smiles

O=C(C1=CC(C(N(CC2=CC=CC(OC3=CC=CC=C3)=C2)[C@H]4CCCC5=C4C=CC=C5)=O)=C(C(O)=O)C=C1C(O)=O)O

Molecular Formula

C33H27NO8

Molecular Weight

565.57

Precautions

H302, H315, H319, H335

References & Citations

[1]Jarvis MF, et, al. A-317491, a novel potent and selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, reduces chronic inflammatory and neuropathic pain in the rat. Proc Natl Acad Sci U S A. 2002 Dec 24;99 (26) :17179-84.|[2]Wu G, et, al. A-317491, a selective P2X3/P2X2/3 receptor antagonist, reverses inflammatory mechanical hyperalgesia through action at peripheral receptors in rats. Eur J Pharmacol. 2004 Nov 3;504 (1-2) :45-53.