rev-erbα

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.

SR8278 is an REV-ERBα antagonist(EC50 = 0.47 µM), blocking activation of the receptor by the synthetic agonist GSK 4112

GSK4112 (SR6452) is a Rev-erbα agonist with EC50 of 0.4 μM, also is a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα.

SR-29065 is a selective agonist of REV-ERBα, utilized in the research of autoimmune disorders [1].

GSK2945 hydrochloride is a tertiary amine and a highly specific antagonist of Rev-erbα/REV-ERBα (mouse/human reverse erythropoietic virus α) with an EC50 value of 21.5 μM and 20.8 μM, respectively.GSK2945 hydrochloride increases cholesterol 7α-hydroxylase ( The EC50 values were 21 μM and 20 μM, respectively.

STL1267, a potent REV-ERB agonist capable of crossing the blood-brain barrier, exhibits a K i value of 0.16 µM for REV-ERBα without demonstrating cytotoxicity. It effectively inhibits the gene expression of BMAL1.

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.

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.

GSK2945 hydrochloride is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist (EC50s: 21.5 μM and 20.8 μM). It enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.

GSK2945 is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist (EC50s: 21.5 μM and 20.8 μM). It enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.

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