您好，欢迎来到化工原料网！ [登录] [免费注册]
化工原料网
发布求购
位置：首页 > 产品库 > Englerin A
立即咨询
咨询类型：
     
*姓名：
*电话：
*单位：
Email：
*留言内容：
请详细说明您的需求。
*验证码：
 
Englerin A
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Englerin A图片
CAS NO:1094250-15-3
包装:5mg
市场价:12150元

产品介绍
Englerin A 是一种有效和选择性的 TRPC4 和 TRPC5 通道的活化剂，EC50 值分别为 11.2 和 7.6 nM。Englerin A 通过增加 Ca2+ 内流和 Ca2+ 细胞超负荷来诱导肾癌细胞死亡。
Cas No.1094250-15-3
别名恩格林A
分子式C26H34O6
分子量442.54
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca2+ influx and Ca2+ cell overload[1][2][3].

Englerin A (0.15-2500 nM; 48 h) characteristic concentration-dependent suppresses cells growth of the A-498 cells treated with the control siRNA while has little effect on the growth of cells treated with TRPC4 siRNAs[3].Englerin A (0.001nM-10 μM; 48 h) inhibits cells viability in HEK293T cells overexpressing TRPC5[3].Englerin A (3 nM; 1-240 s) evokes sustained elevation of the intracellular Ca2+ concentration within 1 min in HEK 293 cells over-expressing human TRPC4[1].Englerin A (0.1-1000 nM; 1-300 s) evokes intracellular Ca2+ elevations in A498 cells as well with an EC50 of 10 nM[1].

Englerin A (5 mg/kg; i.p daily except Sunday) markedly inhibits tumor growth during the 2-week treatment period in mice[4].

[1]. Akbulut Y, et, al. (-)-Englerin A is a potent and selective activator of TRPC4 and TRPC5 calcium channels. Angew Chem Int Ed Engl. 2015 Mar 16;54(12):3787-91.
[2]. Rubaiy HN, et, al. Identification of an (-)-englerin A analogue, which antagonizes (-)-englerin A at TRPC1/4/5 channels. Br J Pharmacol. 2018 Mar; 175(5):830-839.
[3]. Carson C, et, al. Englerin A Agonizes the TRPC4/C5 Cation Channels to Inhibit Tumor Cell Line Proliferation. PLoS One. 2015 Jun 22;10(6):e0127498.
[4]. Sourbier C, et, al. Englerin A stimulates PKCθ to inhibit insulin signaling and to simultaneously activate HSF1: pharmacologically induced synthetic lethality. Cancer Cell. 2013 Feb 11;23(2):228-37.