GSK2945,1438071-12-5

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GSK2945

CAS No. : 1438071-12-5

MCE 国际站：GSK2945

产品活性：GSK2945 是一类叔胺，是一种高度特异性的 Rev-erbα/REV-ERBα (小鼠/人反向成红细胞病病毒α) 拮抗剂， 其 EC₅₀ 值分别为 21.5 μM 和 20.8 μM。GSK2945 可增强胆固醇 7α-羟化酶 (CYP7A1) 水平和胆固醇代谢。

研究领域：Metabolic Enzyme/Protease

作用靶点：Cytochrome P450

In Vitro: GSK2945 dose-dependently enhances the transcriptional activity of Rev-erbα and a Bmal1 (a target gene of REV-ERBs) luciferase reporter (EC₅₀ of 2.05 μM).
GSK2945 (20 μM; 12 hours and 24 hours; mouse and human primary hepatocytes) treatment increases levels of Cyp7a1/CYP7A1 in mouse and human primary hepatocytes. GSK2945 (20 μM) treatment also increases Lrh-1/LRH-1 (a known hepatic activator of Cyp7a1/CYP7A1) mRNA and protein.

In Vivo: GSK2945 (0-10 mg/kg; intraperitoneal injection; twice every day; for 7 days; male C57BL/6 mice) treatment increases hepatic mouse cholesterol 7α-hydroxylase (Cyp7a1) level and lowers plasma cholesterol in wild-type mice.

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