SR8278 (SR-8278; SR 8278) is a novel, potent, synthetic and competitive Rev-Erbα antagonist with the potential for treating Duchenne muscular dystrophy (DMD). In mdx mice SR8278 increased lean mass and muscle function, and decreased muscle fibrosis and muscle protein degradation. SR8278 inhibits Rev-Erbα transcriptional repression with an EC50 of 0.47 μM. REV-ERBα is a member of the nuclear receptor superfamily that functions as a receptor for the porphoryin heme. REV-ERBα suppresses transcription of its target genes in a heme-dependent manner. SR8278 also blocks activity of Rev-Erbα agonist GSK 4112 in HEK293 cells. SR8278 increases expression of glucose-regulating genes, G6Pase and PEPCK in HepG2 cells.

纯度：≥98%

CAS：1254944-66-5