rev-erbbβ

SR9009 (Stenabolic), a REV-ERB agonist, increases the constitutive repression of genes regulated by REV-ERBα ERBβ (IC50: 670 800 nM). Through activation of REV-ERB, SR9009 can decrease circadian locomotor activity during the dark phase and alter the expression pattern of core clock genes in the hypothalami of mice. The circadian pattern of expression of an array of metabolic genes in the liver, skeletal muscle, and adipose tissue was also altered in mice exposed to SR9009, resulting in increased energy expenditure. In Diet-induced obese mice, SR9009 (100 mg kg, i.p., b.i.d., for 30 days) could decrease fat mass and markedly improve dyslipidemia and hyperglycemia.

SR9011 is a REV-ERB agonist (IC50: 790 nM, REV-ERBα; IC50: 560 nM, REV-ERBβ).

SR9011 hydrochloride is a REV-ERBα β agonist, exhibiting IC50 values of 790 nM for REV-ERBα and 560 nM for REV-ERBβ.