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(E/Z)-GSK5182
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。
(E/Z)-GSK5182图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
(E/Z)-GSK5182 是 (E)-GSK5182 和 (Z)-GSK5182 的消旋体。GSK5182 是一种高效选择性,具有口服活性的 ERRγ 反向激动剂,其 IC50 值为 79 nM。GSK5182 还能增加肝癌细胞中 reactive oxyen species (ROS) 的产生。
Canonical SMILESOCCC/C(C1=CC=CC=C1)=C(C2=CC=C(C=C2)OCCN(C)C)\C3=CC=C(C=C3)O
分子式C27H31NO3
分子量417.54
溶解度DMSO: 100 mg/mL (239.50 mM); Water:< 0.1 mg/mL (insoluble)
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

(E/Z)-GSK5182 is a racemic compound of (E)-GSK5182 and (Z)-GSK5182 isomers. GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM[1]. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma[1][2][3].

[1]. Kim JH, et al. Estrogen-related receptor γ is upregulated in liver cancer and its inhibition suppresses livercancer cell proliferation via induction of p21 and p27. Exp Mol Med. 2016 Mar 4;48:e213. [2]. Misra J, et al. ERRγ: a Junior Orphan with a Senior Role in Metabolism. Trends Endocrinol Metab. 2017 Apr;28(4):261-272. [3]. Kim DK, et al. Inverse agonist of nuclear receptor ERRγ mediates antidiabetic effect through inhibition of hepatic gluconeogenesis. Diabetes. 2013 Sep;62(9):3093-102.