rev-erbβ

SR10067 is a potent, selective and brain penetrant agonist of Rev-Erbα/β(IC50 of 160 and 170 nM for Rev-Erbβ and Rev-Erbα, respectively),has anxiolytic activity.

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 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.

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

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.

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 hydrochloride is a REV-ERBα/β agonist, exhibiting an IC50 value of 790 nM for REV-ERBα and 560 nM for REV-ERBβ.