生物活性分子抑制剂A-804598

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A-804598  纯度: 98.77%

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。

A-804598

A-804598 Chemical Structure

CAS No. : 1125758-85-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥825 In-stock
5 mg ¥750 In-stock
10 mg ¥1300 In-stock
25 mg ¥2800 In-stock
50 mg ¥4500 In-stock
100 mg ¥7500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

A-804598 相关产品

相关化合物库:

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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[1].

IC50 & Target

IC50: 9 nM (mouse P2X7 receptor), 10 nM (rat P2X7 receptor), 11 nM (human P2X7 receptor)[1]

体外研究
(In Vitro)

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[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[2]

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[3].

上海金畔生物科技有限公司 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 [3]
Dosage: 30 mg/kg
Administration: Intraperitoneal injection; five times a week
Result: Decreased SQSTM1/p62 expression.

分子量

315.37

Formula

C19H17N5

CAS 号

1125758-85-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Donnelly-Roberts DL et al. [3H]A-804598 ([3H]2-cyano-1-[(1S)-1-phenylethyl]-3-quinolin-5-ylguanidine) is a novel, potent, and selective antagonist radioligand for P2X7 receptors. Neuropharmacology, 2009 Jan, 56(1):223-9.

    [2]. Yingbo He et al. The role of microglial P2X7: modulation of cell death and cytokine release. Neuroinflammation, 2017 Jul, 14(1):135.

    [3]. Paola Fabbrizio et al. P2X7 Receptor Activation Modulates Autophagy in SOD1-G93A Mouse Microglia.Cell Neurosci, 2017 Aug, 11:249.

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