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GSK2945 hydrochloride (1438071-12-5 free base)

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GSK2945 hydrochloride (1438071-12-5 free base)

Catalog No. T11490L

GSK2945 hydrochloride 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.

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Pack Size	Price	Availability
5 mg	$311	Backorder
10 mg	$486	Backorder
50 mg	$1,454	Backorder
100 mg	$1,981	Backorder

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Product Introduction

Bioactivity

Description	GSK2945 hydrochloride 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) treatment also increases Lrh-1/LRH-1 (a known hepatic activator of Cyp7a1/CYP7A1) mRNA and protein.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). 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.
In vivo	GSK2945 treatment increases hepatic mouse cholesterol 7α-hydroxylase (Cyp7a1) level and lowers plasma cholesterol in wild-type mice.
Alias	GSK2945 hydrochloride

Chemical Properties

Molecular Weight	457.8
Formula	C20H19Cl3N2O2S
Cas No.

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

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mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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Keywords

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