SR9011 представляет собой мощный и специфический синтетический агонист REV-ERB, который связывается с REV-ERB-α с EC50 ~790 нМ и REV-ERB-β с EC50 ~560 нМ.. Он также имеет хорошее воздействие на плазму/мозг in vivo.. Ядерные рецепторы REV-ERB-α и REV-ERB-β играют важную роль в регуляции экспрессии белков основных часов., ритмы активности и обмена веществ.
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