A-804598|cas:1125758-85-1|西域试剂

A-804598,98.77%

产品编号：Bellancom-100483| CAS NO：1125758-85-1| 分子式：C₁₉H₁₇N₅| 分子量：315.37

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-100483	￥750.00	杭州北京（现货）
Bellancom-100483	￥1300.00	杭州北京（现货）
Bellancom-100483	￥2800.00	杭州北京（现货）
Bellancom-100483	￥4500.00	杭州北京（现货）
Bellancom-100483	￥7500.00	杭州北京（现货）

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A-804598

产品介绍

A-804598 是一个 CNS 渗透，竞争性和选择性的 P2X7 受体拮抗剂，作用于小鼠，大鼠和人的 P2X7 受体，IC₅₀s 分别是 9 nM, 10 nM 和 11 nM。

生物活性

A-804598 is a CNS penetrant, competitive and selective P2X7 receptor antagonist with IC₅₀s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively.

体外研究

Pre-incubation with A-804598 (0.1-10 μM; 1 hour) significantly attenuates BzATP-induced cell loss in a concentration-dependent manner. 3 μM A-804598 exhibits the greatest protective effect against BzATP-induced cytotoxicity.

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

Cell Cytotoxicity Assay

Cell Line:	microglial cell
Concentration:	0.1, 0.3, 1, 3, 10 μM
Incubation Time:	1 hour
Result:	Protected against BzATP-induced cytotoxicity in both inactivated and activated microglia.

体内研究
(In Vivo)

A chroni treatment with A-804598 (intraperitoneal injection; 30 mg/kg; five times a week) decreases the expression of LC3B-II and SQSTM1/p62 in lumbar spinal cord at end stage of disease.

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

Animal Model:	Adult B6.Cg-Tg (SOD1-G93A) 1Gur/J female mice
Dosage:	30 mg/kg
Administration:	Intraperitoneal injection; five times a week
Result:	Decreased SQSTM1/p62 expression.

体内研究

A chroni treatment with A-804598 (intraperitoneal injection; 30 mg/kg; five times a week) decreases the expression of LC3B-II and SQSTM1/p62 in lumbar spinal cord at end stage of disease.

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

Animal Model:	Adult B6.Cg-Tg (SOD1-G93A) 1Gur/J female mice
Dosage:	30 mg/kg
Administration:	Intraperitoneal injection; five times a week
Result:	Decreased SQSTM1/p62 expression.

体内研究

A chroni treatment with A-804598 (intraperitoneal injection; 30 mg/kg; five times a week) decreases the expression of LC3B-II and SQSTM1/p62 in lumbar spinal cord at end stage of disease.

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

Animal Model:	Adult B6.Cg-Tg (SOD1-G93A) 1Gur/J female mice
Dosage:	30 mg/kg
Administration:	Intraperitoneal injection; five times a week
Result:	Decreased SQSTM1/p62 expression.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 32 mg/mL (101.47 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1709 mL	15.8544 mL	31.7088 mL
5 mM	0.6342 mL	3.1709 mL	6.3418 mL
10 mM	0.3171 mL	1.5854 mL	3.1709 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。-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

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (7.93 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.93 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (7.93 mM); Clear solution; Need ultrasonic

此方案可获得 2.5 mg/mL (7.93 mM) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.93 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.93 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。