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Submit ReviewA 317491 sodium salt is a selective, high affinity non-nucleotide P2X3 and P2X2/3 receptor antagonist (Ki values are 9, 22, 22 and 92 nM at human P2X2/3, rat P2X3, human P2X3 and rat P2X2/3, respectively); blocks recombinant human and rat P2X3 and P2X2/3 receptor-mediated calcium flux (Ki = 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.
A 317491 sodium salt is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 609.54 |
公式 | C33H25NO8Na2 |
储存 | Store at -20°C |
纯度 | ≥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] |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 60.95 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.64 mL | 8.2 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 |
参考文献是支持产品生物活性的出版物。
Jarvis et al (2002) 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.Nat.Acad.Sci.USA 99 17179 PMID: 12482951
McGaraughty et al (2003) Effects of A-317491, a novel and selective P2X3/P2X2/3 receptor antagonist, on neuropathic, inflammatory and chemogenic nociception following intrathecal and intraplantar administration. Br.J.Pharmacol. 140 1381 PMID: 14623769
McGaraughty et al (2005) 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. 146 180 PMID: 16041397
Mansoor et al (2016) X-ray structures define human P2X3 receptor gating cycle and antagonist action. Nature 538 66 PMID: 27626375
Neelands et al (2003) 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. 140 202 PMID: 12967950
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