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GSK2945

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Catalog No. T11490Cas No. 1438071-12-5

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.

GSK2945

GSK2945

😃Good
Catalog No. T11490Cas No. 1438071-12-5
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 SizePriceAvailabilityQuantity
25 mg$1,5206-8 weeks
50 mg$1,9806-8 weeks
100 mg$2,5006-8 weeks
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Product Introduction

Bioactivity
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.
Chemical Properties
Molecular Weight421.34
FormulaC20H18Cl2N2O2S
Cas No.1438071-12-5
Relative Density.1.363 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.3734 mL11.8669 mL23.7338 mL118.6690 mL
5 mM0.4747 mL2.3734 mL4.7468 mL23.7338 mL
10 mM0.2373 mL1.1867 mL2.3734 mL11.8669 mL
20 mM0.1187 mL0.5933 mL1.1867 mL5.9335 mL
50 mM0.0475 mL0.2373 mL0.4747 mL2.3734 mL
100 mM0.0237 mL0.1187 mL0.2373 mL1.1867 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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