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
