BzATP triethylammonium salt

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BzATP triethylammonium salt  纯度: ≥95.0%

BzATP triethylammonium salt 是一种 P2X 受体激动剂,对 P2X1,P2X2,P2X3,P2X2/3,P2X4 和 P2X7 的 pEC50 分别为 8.74,5.26,7.10,7.50, 6.19,6.31 和 5.33。BzATP triethylammonium salt 对 P2X7 受体有效,对大鼠 P2X7 和小鼠 P2X7 的EC50 分别为 3.6 μM 和 285 μM。

BzATP triethylammonium salt

BzATP triethylammonium salt Chemical Structure

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生物活性

BzATP triethylammonium salt acts as a P2X receptor agonist with pEC50s of 8.74, 5.26, 7.10, 7.50, 6.19, 6.31, 5.33 for P2X1, P2X2, P2X3, P2X2/3, P2X4 and P2X7, respectively[1]. BzATP triethylammonium salt is potent at P2X7 receptors with EC50s of 3.6 μM and 285 μM for rat P2X7 and mouse P2X7, respectively[2].

IC50 & Target

pEC50: 8.74 (P2X1), 5.26 (P2X2), 7.10 (P2X3), 6.19 (P2X2/3), 6.31 (P2X4), 5.33 (P2X7)[1]
EC50 3.6 μM (rat P2X7); 285 μM (mouse P2X7)[2]

体外研究
(In Vitro)

BzATP (10-1000 μM; 24 h) promotes the proliferation and migration of U87 and U251 glioma cells[3].
P2X7R protein expression is induced by BzATP (100 μM; 6-48 h) in human glioma cells[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.

Cell Proliferation Assay[3]

Cell Line: U87 and U251 glioma cells
Concentration: 5, 10, 50, 100, 500 and 1000 μM
Incubation Time: 2, 6, 12, 24, 48 and 72 hours
Result: The proliferation of U87 and U251 glioma cell lines was significantly increased in the presence of 10-1000 uM and 100-1000 μM, respectively.
The peak of cell proliferation of both U87 and U251 cell lines was at 100 μM.
The optimal incubation time is 24 hours in both U87 and U251 cells lines.

Western Blot Analysis[3]

Cell Line: U87 and U251 glioma cells
Concentration: 100 μM
Incubation Time: 6-48 hours
Result: Induced the upregulation of P2X7R.

体内研究
(In Vivo)

BzATP (5 mg/kg) significantly promotes P2X7R expression in the intestines compared with intestines in the sham group and the control group after cecal ligation and puncture (CLP) induction[4].

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: Male 2-month-old C57BL/6 mice (each weighing between 20 and 25 g)[4]
Dosage: 5 mg/kg
Administration: Injected through the intraperitoneal route
Result: At 48 hours, mice in the treated group and control group exhibited mortalities of 91% and 86%, respectively.

分子量

1018.97

Formula

C84H138N16O30P6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : 250 mg/mL (245.35 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.9814 mL 4.9069 mL 9.8138 mL
5 mM 0.1963 mL 0.9814 mL 1.9628 mL
10 mM 0.0981 mL 0.4907 mL 0.9814 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。

参考文献
  • [1]. B R Bianchi, et al. Pharmacological characterization of recombinant human and rat P2X receptor subtypes. Eur J Pharmacol. 1999 Jul 2;376(1-2):127-38.

    [2]. Mark T Young, et al. Amino acid residues in the P2X7 receptor that mediate differential sensitivity to ATP and BzATP. Mol Pharmacol. 2007 Jan;71(1):92-100.

    [3]. Zhenhua Ji, et al. Involvement of P2X 7 Receptor in Proliferation and Migration of Human Glioma Cells. Biomed Res Int. 2018 Jan 9;2018:8591397.

    [4]. Xiuwen Wu, et al. Systemic blockade of P2X7 receptor protects against sepsis-induced intestinal barrier disruption. Sci Rep. 2017 Jun 29;7(1):4364.

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