SR8278

SR8278 is a synthetic small molecule that acts as an antagonist of the nuclear hormone receptors REV-ERBα and REV-ERBβ. It was the first synthetic antagonist identified for REV-ERBs and is mainly used as a research tool to probe REV-ERB functions. SR8278 binds to the orthosteric pocket of REV-ERBα, blocking its transcriptional repressor activity, and thus modulates physiological processes such as circadian rhythm, metabolism, inflammation, muscle generation, and mood regulation[1][2][3][4][5]. In preclinical studies, SR8278 has been shown to increase lean muscle mass, decrease muscle fibrosis, and stimulate muscle regeneration in models of Duchenne muscular dystrophy, likely through REV-ERB antagonism and Wnt signaling pathway activation[1][2]. It also exhibits antidepressant and anxiolytic effects in Parkinson's disease models with circadian mood disturbances, supporting its potential for chronotherapy of mood disorders[3][6]. The compound is primarily used in vitro and in vivo as a chemical probe due to its poor pharmacokinetic properties and very short plasma half-life[1].

Other names

SR8278SR-8278SR 8278