1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. GSK2945

GSK2945 

Cat. No.: HY-117147
Handling Instructions

GSK2945 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. GSK2945 enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.

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GSK2945 Chemical Structure

GSK2945 Chemical Structure

CAS No. : 1438071-12-5

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Description

GSK2945 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. GSK2945 enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism[1].

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)[1].
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[1].

RT-PCR[1]

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.
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[1].

Animal Model: Male C57BL/6 mice (8-10 weeks of age)[1]
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.
Molecular Weight

421.34

Formula

C₂₀H₁₈Cl₂N₂O₂S

CAS No.

1438071-12-5

SMILES

O=[N+](C1=CC=C(CN(CC2=CC=C(Cl)C=C2C)CC3=CC=C(Cl)C=C3)S1)[O-]

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

GSK2945GSK 2945GSK-2945Cytochrome P450CYPsInhibitorinhibitorinhibit

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GSK2945
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