| 中文名称 |
A-317491 sodium salt hydrate
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| 英文名称 |
A-317491 sodium salt hydrate
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| 包装储存 |
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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| 详情描述 |
A-317491 sodium salt hydrate 是一种有效,选择性和非核苷酸的 P2X3 和 P2X2/3 受体的拮抗剂,对 hP2X3,rP2X3,hP2X2/3 和 rP2X2/3 的 Ki 值分别为 22,22,9 和 92 nM。A-317491 sodium salt hydrate 对其他 P2 受体和神经递质受体,离子通道以及酶具有高度选择性 (IC50>10 μM)。A-317491 sodium salt hydrate 通过阻断 P2X3 和 P2X2/3 受体介导的钙通量减轻炎性和神经性疼痛。
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| 产品详情 |
A-317491 sodium salt hydrate 是一种有效,选择性和非核苷酸的 P2X3 和 P2X2/3 受体的拮抗剂,对 hP2X3,rP2X3,hP2X2/3 和 rP2X2/3 的 Ki 值分别为 22,22,9 和 92 nM。A-317491 sodium salt hydrate 对其他 P2 受体和神经递质受体,离子通道以及酶具有高度选择性 (IC50>10 μM)。A-317491 sodium salt hydrate 通过阻断 P2X3 和 P2X2/3 受体介导的钙通量减轻炎性和神经性疼痛。
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| 生物活性 |
A-317491 sodium salt hydrate is a potent, selective and non-nucleotide antagonist of P2X 3 and P2X 2/3 receptors, with K i s of 22, 22, 9, and 92 nM for hP2X 3 , rP2X 3 , hP2X 2/3 , and rP2X 2/3 , respectively. A-317491 sodium salt hydrate is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 sodium salt hydrate reduces inflammatory and neuropathic pain by blocking P2X 3 and P2X 2/3 receptor-mediated calcium flux.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
P2X3 Receptor
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| 体外研究(In Vitro) |
A-317491 potently blocks recombinant human and rat P2X3 and P2X2/3 receptor-mediated calcium flux (Ki=22-92 nM) .A-317491 (1 nM-10 μM) produces a concentration-dependent block of dorsal root ganglion (DRG) currents with an IC50 of 15 nM. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 体内研究(In Vivo) |
A-317491 (0.1-30 mg/kg; a single s.c.) dose-dependently reverses inflammatory mechanical hyperalgesia in rats.
A-317491 (3-30 mg/kg; a single .v.) exhibits the plasma half-life (7.38 h), clearance rate (1.83 L/h/kg), and volume of distribution (0.17 L/kg). has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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| 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.
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| 溶解度数据 |
In Vitro: H2O : 100 mg/mL (164.86 mM; Need ultrasonic)配制储备液
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[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.
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。