BzATP (triethylammonium salt)

国际站：BzATP (triethylammonium salt)

品牌：MedChemExpress (MCE)

存储条件：-20°C, sealed storage, away from moisture

生物活性：BzATP 三乙基铵盐作为 P2X 受体 激动剂，对 P2X1 的 pEC₅₀ 为 8.74、5.26、7.10、7.50、6.19、6.31、5.33 , P2X2, P2X3, P2X2/3, P2X4 和 P2X7, 分别^[1]. BzATP 三乙铵盐对 P2X7 受体有效，对大鼠 P2X7 和小鼠 P2X7 的 EC₅₀ 分别为 3.6 μM 和 285 μM^[2] . IC50 和目标：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（大鼠 P2X7）； 285 μM（小鼠 P2X7）^[2]

体外：BzATP (10-1000 μM; 24 h) 促进 U87 和 U251 胶质瘤细胞的增殖和迁移^[3]。P2X7R 蛋白表达由 BzATP (100 μM; 6-48 h) 在人类神经胶质瘤细胞中^[3].

体内：与假手术组和对照组相比，BzATP (5 mg/kg) 显着促进盲肠结扎穿孔 (CLP) 诱导后肠道中 P2X7R 的表达^[4]。

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.