(E/Z)-GSK5182

(E/Z)-GSK5182 (GSK5182(Z/E)) 是 (E)-GSK5182 和 (Z)-GSK5182 的外消旋体。GSK5182 是一种具有高效选择性和口服活性的ERRγ的反向激动剂,其IC50值为 79 nM。GSK5182 还诱导肝癌细胞中活性氧 (ROS)的产生。

CAS号

T7709

分子式

C27H31NO3

主要靶点

ROS|Estrogen/progestogen Receptor

仅限科研使用

Cat No : CM08809

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Synonyms

GSK5182(Z/E)



产品信息

(E/Z)-GSK5182 is a racemate 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 IC 50 of 79 nM [1]. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma [1] [2] [3].

CAS号 T7709
分子式 C27H31NO3
主要靶点 ROS|Estrogen/progestogen Receptor
主要通路 内分泌与激素|免疫与炎症
分子量 417.54
纯度 98.83%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 GSK5182(Z/E)

溶解度

DMSO:95 mg/mL (227.52 mM),Sonification is recommended.

参考文献

1.Misra J, et al. ERRγ: a Junior Orphan with a Senior Role in Metabolism. Trends Endocrinol Metab. 2017 Apr;28(4):261-272.
2.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.
3.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.

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