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CAS No.: 475205-49-3

A-317491 Catalog No. CSN18291

Synonyms: A-317491

A-317491 is a potent and selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors with Ki values of 22 nM and 9 nM for human P2X3 and P2X2/3 receptors.

规格	价格	促销价格	库存	数量

400-920-2911

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生物活性

实验方案

技术信息

生物活性

描述A-317491 is a potent and selective non-nucleotide antagonist of P2X₃ and P2X_2/3 receptors with Ki values of 22–92 nM for blocking recombinant human and rat P2X₃ and P2X_2/3 receptor-mediated calcium flux. It also blocked native P2X₃ and P2X_2/3 receptors in rat dorsal root ganglion neurons. A-317491 dose-dependently reduced complete Freund's adjuvant-induced thermal hyperalgesia in the rat with ED50 value of 30μmol/kg, s.c., as well as attenuated both thermal hyperalgesia and mechanical allodynia after chronic nerve constriction injury with ED50 value of 10-15μmol/kg.
作用机制A-317491 is a competitive antagonist which can stabilize the apo/resting state of P2X₃.^[2]^[3]
动物研究
剂量
Rat: 3 mg/kg - 30 mg/kg^[4] (s.c.); 20 mg/kg , 50 mg/kg (i.v.)

给药途径
s.c., i.v.
参考文献

动物研究
剂量	Rat: 3 mg/kg - 30 mg/kg^[4] (s.c.); 20 mg/kg , 50 mg/kg (i.v.)
给药途径	s.c., i.v.

[1] Jarvis MF, Burgard EC, 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. Epub 2002 Dec 13.
[2] Neelands TR, Burgard EC, et al. 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 Sep;140(1):202-10. Epub 2003 Jul 29.
[3] Mansoor SE, Lü W, et al. X-ray structures define human P2X(3) receptor gating cycle and antagonist action. Nature. 2016 Oct 6;538(7623):66-71.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7681 mL
- 8.8406 mL
- 17.6813 mL
- 5 mM
- 0.3536 mL
- 1.7681 mL
- 3.5363 mL
- 10 mM
- 0.1768 mL
- 0.8841 mL
- 1.7681 mL

技术信息

CAS号

475205-49-3

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C33H27NO8

运输

蓝冰

分子量

565.57

别名

A-317491

溶解度

DMSO	50.0 mg/mL (88.4 mM)
Water	insoluble

动物实验配方

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