A-317491 sodium salt hydrate|西域试剂

A-317491 sodium salt hydrate,99.88%

产品编号：Bellancom-15568A| 分子式：C₃₃H₂₉NNaO₉| 分子量：606.57

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-15568A	￥949.00	杭州北京（现货）
Bellancom-15568A	￥1414.00	杭州北京（现货）
Bellancom-15568A	￥4780.00	杭州北京（现货）

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A-317491 sodium salt hydrate

产品介绍

A-317491 sodium salt hydrate 是一种有效，选择性和非核苷酸的 P2X₃ 和 P2X_2/3 受体的拮抗剂，对 hP2X₃，rP2X₃，hP2X_2/3 和 rP2X_2/3 的 K_i 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 P2X_2/3 受体介导的钙通量减轻炎性和神经性疼痛。

生物活性

A-317491 sodium salt hydrate is a potent, selective and non-nucleotide antagonist of P2X₃ and P2X_2/3 receptors, with K_is of 22, 22, 9, and 92 nM for hP2X₃, rP2X₃, 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 P2X₃ and P2X_2/3 receptor-mediated calcium flux.

体外研究

A-317491 potently blocks recombinant human and rat P2X₃ and P2X_2/3 receptor-mediated calcium flux (K_i=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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male adult Sprague-Dawley rats received an intraplantar injection of Freund's complete adjuvant
Dosage:	0.1, 1, 3, 10, 30 mg/kg
Administration:	A single s.c.
Result:	Produced a dose-dependent reduction in mechanical hyperalgesia 1 h, 3 h and 5 h post-administration.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male adult Sprague-Dawley rats received an intraplantar injection of Freund's complete adjuvant
Dosage:	0.1, 1, 3, 10, 30 mg/kg
Administration:	A single s.c.
Result:	Produced a dose-dependent reduction in mechanical hyperalgesia 1 h, 3 h and 5 h post-administration.

性状

Solid

溶解性数据

In Vitro:

H₂O : 100 mg/mL (164.86 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6486 mL	8.2431 mL	16.4861 mL
5 mM	0.3297 mL	1.6486 mL	3.2972 mL
10 mM	0.1649 mL	0.8243 mL	1.6486 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶