SR9011 es un agonista sintético potente y específico de REV-ERB que se une a REV-ERB-α con una EC50 ~790 nM y a REV-ERB-β con EC50 ~560 nM. También tiene una buena exposición al plasma/cerebro in vivo.. Los receptores nucleares REV-ERB-α y REV-ERB-β desempeñan un papel integral en la regulación de la expresión de las proteínas del reloj central., Ritmos impulsores en la actividad y el metabolismo..
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