GSK5182

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GSK5182 是一种高选择性逆雌激素相关受体 γ 激动剂 (IC50: 79 nM)。

GSK5182 is a highly selective inverse estrogen-related receptor γ agonist (IC50 : 79 nM)?.(In Vitro):GSK5182 (0-20 μM; 0-hours; PLC/PRF/5 cells) treatment leads to a significant and dose-dependent reduction in the number of proliferating PLC/PRF/5 cells.GSK5182 (0-20 μM; 24 hours; PLC/PRF/5 cells) treatment also causes a dose-dependent increase in the expression of p21 and p27 while at the same time reducing the level of phosphorylated retinoblastoma protein (p-pRb).GSK5182 (10-20 μM; PLC/PRF/5 cells) treatment induces cell cycle arrest at G1 phase, which in turn induces a corresponding dose-dependent reduction in the percentage of cells in S phase.(In Vivo):GSK5182 (40 mg/kg; intraperitoneal injection; every day; 25 or 30 days; db/db mice, diet-induced obesity mice) specifically inhibits the transcriptional activity of ERRγ, and suppresses hepatic glucose production through inhibition of hepatic gluconeogenesis. GSK5182 elicits anti-diabetic effects in mouse models via negative regulation of the hepatic gluconeogenesis program. GSK5182 normalizes hyperglycemia mainly through inhibition of hepatic glucose production.

GSK5182 (0-20 μM; 0-hours; PLC/PRF/5 cells) treatment leads to a significant and dose-dependent reduction in the number of proliferating PLC/PRF/5 cells.GSK5182 (0-20 μM; 24 hours; PLC/PRF/5 cells) treatment also causes a dose-dependent increase in the expression of p21 and p27 while at the same time reducing the level of phosphorylated retinoblastoma protein (p-pRb).GSK5182 (10-20 μM; PLC/PRF/5 cells) treatment induces cell cycle arrest at G1 phase, which in turn induces a corresponding dose-dependent reduction in the percentage of cells in S phase. Cell Proliferation Assay 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 Result:Led to a significant and dose-dependent reduction in the number of proliferating PLC/PRF/5 cells.Western Blot Analysis Cell Line:The human hepatoma cell line PLC/PRF/5 Concentration:0 μM, 10 μM, 20 μM Incubation Time:24 hours Result:Caused a dose-dependent increase in the expression of p21 and p27 while at the same time reducing the level of p-pRb. Cell Cycle Analysis Cell Line:The human hepatoma cell line PLC/PRF/5 Concentration:10 μM, 20 μM Incubation Time:Result:Induced cell cycle arrest.

GSK5182 (40 mg/kg; intraperitoneal injection; every day; 25 or 30 days; db/db mice, diet-induced obesity mice) specifically inhibits the transcriptional activity of ERRγ, and suppresses hepatic glucose production through inhibition of hepatic gluconeogenesis. GSK5182 elicits anti-diabetic effects in mouse models via negative regulation of the hepatic gluconeogenesis program. GSK5182 normalizes hyperglycemia mainly through inhibition of hepatic glucose production. Animal Model:db/db mice (male, 7-12-week-old), diet-induced obesity (DIO) mice Dosage:40 mg/kg Administration:Intraperitoneal injection; every day; 30 days for db/db mice, 25 days for DIO mice Result:Inhibited the transcriptional activity of ERRγ, suppressed hepatic glucose production through inhibition of hepatic gluconeogenesis.

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Endocrinology/Hormones

Estrogen Receptor/ERR

ERRγ

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877387-37-6

417.55

C27H31NO3

>98% (HPLC)

In Vitro:?DMSO : 25 mg/mL (59.87 mM)

CN(C)CCOc1ccc(cc1)C(\c1ccc(O)cc1)=C(\CCCO)c1ccccc1

4-[(Z)-1-[4-(2-dimethylaminoethoxy)phenyl]-5-hydroxy-2-phenylpent-1-enyl]phenol

(-20℃)

With Ice Pack

≥ 2 years