REV-ERBα is a nuclear receptor and transcription repressor that coordinates circadian rhythm and metabolic pathways in a heme-dependent manner.{27845,21477} SR 8278 is an antagonist of REV-ERBα (EC50 = 0.47 µM), blocking activation of the receptor by the synthetic agonist GSK 4112 (Item No. 11931).{21477} Moreover, SR 8278 stimulates the expression of two REV-ERBα target genes involved in the regulation of glucose production, glucose 6-phosphatase and phosphoenolpyruvate carboxykinase, in liver cells.{21477} SR 8278 has been used, with GSK 4112, to elucidate the role of REV-ERBα in regulating glucagon secretion in pancreatic alpha cells.{27844}
产品描述
An antagonist of REV-ERBα (EC50 = 0.47 µM), blocking activation of the receptor by the synthetic agonist GSK 4112; stimulates the expression of the REV-ERBα target genes G6Pase and PEPCK in liver cells; used to elucidate the role of REV-ERBα in regulating glucagon secretion in pancreatic alpha cells
