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GSK2945 is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist (EC50s: 21.5 μM and 20.8 μM). It enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,520 | 6-8 weeks | |
50 mg | $1,980 | 6-8 weeks | |
100 mg | $2,500 | 6-8 weeks |
Description | GSK2945 is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist (EC50s: 21.5 μM and 20.8 μM). It enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism. |
In vitro | 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/CYP7A.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) mRNA and protein. |
In vivo | GSK2945 treatment increases hepatic mouse cholesterol 7α-hydroxylase (Cyp7a1) level and lowers plasma cholesterol in wild-type mice. |
Molecular Weight | 421.34 |
Formula | C20H18Cl2N2O2S |
Cas No. | 1438071-12-5 |
Relative Density. | 1.363 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 83.33 mg/mL (197.77 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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