GSK4112

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性小分子 Rev-erbα 激动剂，生化测定中 EC50 为 0.4 uM。

A potent and selective small molecule Rev-erbα agonist with EC50 of 0.4 uM in biochemical assay; mediates the repression of Rev-erbα target gene bmal1 in liver cells, and inhibits and shifts the phase of gluconeogenesis in primary mouse hepatocytes.

GSK4112 (0-100 μM; 1 h) interacts with Rev-erbα with an EC50 value of 0.4 μM.GSK4112 (10 μM; 6 h) represses expression of bmal1 and the target genes associated with the pathway of gluconeogenesis, recruits HDAC3 and modulates the effect of Rev-erbα on oscillation of hepatic gene expression.GSK4112 (10 μM; 16 h) reduces glucose output in murine hepatocytes. RT-PCR Cell Line:HepG2 cell line Concentration:10 μM Incubation Time:6 hours Result:Repressed mRNA levels of bmal1, G6 Pase, PEPCK and PGC1α.

GSK4112 (25 mg/kg; i.p. 0.5 h before Jo2 exposure) attenuates Fas-induced hepatic damage. Animal Model:Male C57BL/6 mice with Fas-induced acute hepatic damage Dosage:25 mg/kg Administration:Intraperitoneal injection; 25 mg/kg; 0.5 h before Jo2 exposure Result:Obviously ameliorated the degree of liver damage, suppressed Jo2-induced ALT and AST increasing, improved the survival rate of mice and suppressed Fas-induced hepatocyte apoptosis.

SR6452 | GSK-4112 | GSK 4112 | SR-6452 | SR 6452

Autophagy

Autophagy

Rev-ErbBα

Metabolic Disease

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1216744-19-2

396.8883

C18H21ClN2O4S

>98% (HPLC)

10 mM in DMSO

O=C(OC(C)(C)C)CN(CC1=CC=C(Cl)C=C1)CC2=CC=C([N+]([O-])=O)S2

Glycine, N-[(4-chlorophenyl)methyl]-N-[(5-nitro-2-thienyl)methyl]-, 1,1-dimethylethyl ester

(-20℃)

With Ice Pack

≥ 2 years