SR9011 potens est ac specifica synthetica REV-ERB agonista, quae obligat ad REV-ERB-α cum EC50 ~ 790 nM et REV-ERB-β cum EC50 ~ 560 nM.. Etiam in vivo plasma bonum habet/expositio cerebri. Receptores nuclei REV-ERB-α et REV-ERB-β partes integrales agunt in moderandis expressionis core horologii servo., driving rhythmi in actione et metabolismi.
Administration of SR9011 alters circadian behavior and the circadian pattern of core clock gene expression in the hypothalami of mice. The circadian expression pattern of an array of metabolic genes in the liver, skeletal muscle and adipose tissue was also altered, resulting in increased energy expenditure.
Treatment of diet-induced obese mice with SR9011 decreased obesity by reducing fat mass and markedly improved dyslipidaemia and hyperglycaemia. These results indicate that synthetic REV-ERB ligands that pharmacologically target the circadian rhythm may be beneficial in the treatment of sleep disorders as well as metabolic