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编 号:F076112
分子式:C18H21ClN2O4S
分子量:396.89
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
GSK4112 (SR6452) is a Rev-erbα agonist with an EC50 value of 0.4 μM. GSK4112 can be used as a chemical tool to probe the function of Rev-erbα in transcriptional repression, regulation of circadian biology, and metabolic pathways.

体内研究:
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.

体外研究:
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.
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