rev-erbβ

SR10067 is a potent, selective, and brain-penetrant agonist of Rev-Erbβ (IC50 = 160 nM) and Rev-Erbα (IC50 = 170 nM) with anxiolytic activity.

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.

ARN5187 is a lysosomal compound, REV-ERB β Ligand. ARN5187 inhibits REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 shows lysosomal efficacy and cytotoxicity, and can induce apoptosis.

SR12418 is a specific REV-ERB synthetic ligand that acts on REV-ERBα (IC50: 68 nM) and REV-ERBβ (IC50: 119 nM) and can be used to study experimental autoimmune encephalomyelitis (EAE) and colitis.

ARN5187 trihydrochloride is a lysosomal REV-ERBβ ligand that inhibits REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 trihydrochloride has lysosomal potency and cytotoxicity and induces apoptosis.