体外研究
GSK2945 dose-dependently enhances the transcriptional activity of Rev-erbα and a Bmal1 (a target gene of REV-ERBs) luciferase reporter (
EC
50
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.
RT-PCR
Cell Line:
Mouse (male, CD1) and human (male, Caucasian) primary hepatocytes
Concentration:
20 μM
Incubation Time:
12 hours and 24 hours
Result:
Led to significant increases in mRNA and protein (at 24-h) expression of Cyp7a1. mRNA and protein (at 24-h) levels of CYP7A1 were increased in human primary hepatocyte. Lrh-1/LRH-1 was upregulated.
体内研究
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.
Animal Model:
Male C57BL/6 mice (8-10 weeks of age)
Dosage:
0 mg/kg or 10 mg/kg
Administration:
Intraperitoneal injection; twice every day; for 7 days
Result:
Increased hepatic mouse cholesterol 7α-hydroxylase (Cyp7a1) level and lowered plasma cholesterol in wild-type mice.
医药
1438071-12-5 N-[(4-氯-2-甲基苯基)甲基]-1-(4-氯苯基)-N-[(5-硝基噻吩-2-基)甲基]甲胺 - 化工 AI 网
