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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。
GSK5182图片
CAS NO:877387-37-6
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议

产品介绍
GSK5182 是高效选择性,具有口服活性的ERRγ反向激动剂,其IC50=79 nM,且不与其他核受体相互作用,包括 ERRα 和 ERα。它还能增加肝癌细胞中reactive oxyen species (ROS)的产生。

产品描述

GSK5182 is a highly selective inverse estrogen-related receptor γ agonist (IC50 : 79 nM)

体外活性

Small interfering RNA (siRNA)-mediated knockdown of ERRγ (siRNA-ERRγ) or an ERRγ inverse agonist, GSK5182, were also used to examine the effects of ERRγ inhibition on the proliferation and growth of a human hepatoma cell line, PLC/PRF/5[1].

体内活性

a hyperinsulinemic-euglycemic clamp study and long-term studies of the antidiabetic effects of GSK5182, the ERRγ-specific inverse agonist, in db/db and DIO mice demonstrated that GSK5182 normalizes hyperglycemia mainly through inhibition of hepatic glucose production[2].

细胞实验

Cell Line:The human hepatoma cell line PLC/PRF/5. Concentration:0 μM, 10 μM, 20 μM. Incubation Time:0 hour, 24 hours, 48 hours, 72 hours

Cas No.

877387-37-6

分子式

C27H31NO3

分子量

417.549

储存和溶解度

DMSO:60 mg/ml (143.7 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years