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Medchemexpress LLC GSK2945 hydrochloride | 98.5% | 457.80 | 100 MG
Supplier: Medchemexpress LLC HY117147A100MG
GSK2945 hydrochloride is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. It enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.
- 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).
- Treatment (20 μM; 12 hours and 24 hours; mouse and human primary hepatocytes) increases levels of Cyp7a1/CYP7A1 in mouse and human primary hepatocytes.
- Treatment (20 μM) also increases Lrh-1/LRH-1 (a known hepatic activator of Cyp7a1/CYP7A1) mRNA and protein.
- Treatment (0-10 mg/kg; intraperitoneal injection; twice every day; for 7 days; male C57BL/6 mice) increases hepatic mouse cholesterol 7α-hydroxylase (Cyp7a1) level and lowers plasma cholesterol in wild-type mice.
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