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• 产品描述： 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

• 靶点： Rev-ErbBα;Autophagy

• 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. 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.

• 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.

• 参考文献：
  1. Grant D, et al. GSK4112, a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα. ACS Chem Biol. 2010 Oct 15;5(10):925-932. 2. Shao R, et al. REV-ERBα Agonist GSK4112 attenuates Fas-induced Acute Hepatic Damage in Mice. Int J Med Sci. 2021 Oct 25;18(16):3831-3838.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.52 ml	12.598 ml	25.196 ml
  5 mM	0.504 ml	2.52 ml	5.039 ml
  10 mM	0.252 ml	1.26 ml	2.52 ml
  50 mM	0.05 ml	0.252 ml	0.504 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *