SR8278

REV-ERBa is a nuclear receptor and transcription repressor that coordinates circadian rhythm and metabolic pathways in a heme-dependent manner.{27845,21477} SR8278 is an antagonist of REV-ERBa (EC50 = 0.47 µM), blocking activation of the receptor by the synthetic agonist GSK 4112 (Item No. 11931).{21477} Moreover, SR8278 stimulates the expression of two REV-ERBa target genes involved in the regulation of glucose production, glucose 6-phosphatase and phosphoenolpyruvate carboxykinase, in liver cells.{21477} SR8278 has been used, with GSK 4112, to elucidate the role of REV-ERBa in regulating glucagon secretion in pancreatic alpha cells.{27844}