SR8278

REV-ERBα is a nuclear receptor and transcription repressor that coordinates circadian rhythm and metabolic pathways in a heme-dependent manner. SR8278 is an antagonist of REV-ERBα (EC₅₀ = 0.47 μM), blocking activation of the receptor by the synthetic agonist GSK 4112 . Moreover, SR8278 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. SR8278 has been used, with GSK 4112, to elucidate the role of REV-ERBα in regulating glucagon secretion in pancreatic alpha cells.

SR 8278 is a synthetic antagonist of the nuclear heme receptor REV-ERB.

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[1] HéLèNE DUEZ  Bart S. Rev-erb-alpha: an integrator of circadian rhythms and metabolism.[J]. Journal of applied physiology, 2009, 107 6: 1972-1980. DOI: 10.1152/japplphysiol.00570.2009
[2] DOUGLAS KOJETIN. Identification of SR8278, a Synthetic Antagonist of the Nuclear Heme Receptor REV-ERB[J]. ACS Chemical Biology, 2010, 6 2: 131-134. DOI: 10.1021/cb1002575
[3] ELAINE VIEIRA. Involvement of the clock gene Rev-erb alpha in the regulation of glucagon secretion in pancreatic alpha-cells.[J]. PLoS ONE, 2013: e69939. DOI: 10.1371/journal.pone.0069939