A-317491

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Chemical Structure| 475205-49-3 同义名 : -
CAS号 : 475205-49-3
货号 : A497149
分子式 : C33H27NO8
纯度 : 99%+
分子量 : 565.57
MDL号 : MFCD28044314
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 45 mg/mL(79.57 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • P2X receptor

    Rat P2X2/3, Ki:92 nM

    Human P2X3, Ki:22 nM
描述 A-317491 exhibits high efficacy and selectivity as a non-nucleotide P2X3 and P2X2/3 receptor blocker, presenting Kis of 22, 22, 9, and 92 nM against hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. Its selective action (IC50>10 μM) spans beyond other P2 receptors and a range of neurotransmitter receptors, ion channels, and enzymes, mitigating inflammatory and neuropathic pain by obstructing P2X3 and P2X2/3 receptor-mediated calcium movement .
作用机制 A-317491 is a competitive antagonist which can stabilize the apo/resting state of P2X3.[2][3]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.77mL

0.35mL

0.18mL

8.84mL

1.77mL

0.88mL

17.68mL

3.54mL

1.77mL
参考文献

[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.