SR-8278 | REV-ERBα antagonist

SR-8278 (125944-66-5) is an antagonist of the nuclear heme receptor, REV-ERB. Blocks the ability of the REV-ERBα agonist, GSK4112, to enhance REV-ERB-dependent repression in a cotransfection assay.¹ Decreases glucagon secretion and intracellular calcium signals in alphaTC1-9 cells and mouse primary alpha cells.² Enhances the expression of bone morphogenetic protein genes in rat uterus endometrium stromal cells.³ Shortens the period of circadian oscillations in mature granulosa cells stimulated with or without LH.⁴

References/Citations:

1) Kojetin et al. (2011), Identification of SR8278,a synthetic antagonist of the nuclear heme receptor REV-ERB; ACS Chem. Biol. 6 131
2) Vieira et al. (2013), Involvement of the Clock Gene Rev-erb alpha in the Regulation of Glucagon Secretion in Pancreatic Alpha-cells; PLoS ONE 8 e69939
3) Tasaki et al. (2015), Inhibitory role of REV-ERBα in the expression of bone morphogenetic protein gene family in rat uterus endometrium stromal cells; Am. J. Physiol. Cell. Physiol., 308 C528
4) Chen et al. (2015), Integration of the nuclear receptor REV-ERBα linked with circadian oscillators in the expressions of Alas1, Pparg1a, and Il6 genes in rat granulosa cells; Chronobiol. Int., 32 739