Product IntroductionBioactivity英文名:
GSK5182描述: 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。
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
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].
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 60 mg/ml (143.7 mM)
关键字:
GSK-5182 |
inhibit |
GSK 5182 |
Reactive Oxygen Species |
Estrogen Receptor/ERR |
GSK5182 |
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