SR8278

REV-ERBalpha is a nuclear receptor and transcription repressor that coordinates circadian rhythm and metabolic pathways in a heme-dependent manner. SR8278 is an antagonist of REV-ERBalpha (EC50 = 0.47 µM), blocking activation of the receptor by the synthetic agonist GSK 4112 (Cay-11931). Moreover, SR8278 stimulates the expression of two REV-ERBalpha target genes involved in the regulation of glucose production, glucose 6-phosphatase and phosphoenolpyruvate carboxykinase, in liver cells. SR8278 has been used, with GSK 4112, to elucidate the role of REV-ERBalpha in regulating glucagon secretion in pancreatic alpha cells.Formal Name: 1,2,3,4-tetrahydro-2-[[5-(methylthio)-2-thienyl]carbonyl]-3-isoquinolinecarboxylic acid, ethyl ester. CAS Number: 1254944-66-5. Molecular Formula: C18H19NO3S2. Formula Weight: 361.5. Purity: >90%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 15 mg/ml, DMSO: 10 mg/ml, Ethanol: 15 mg/ml, Ethanol:PBS (pH 7.2) (1:2): 0.3 mg/ml. lambdamax: 248, 309 nm. SMILES: O=C(OCC)C1N(C(C2=CC=C(SC)S2)=O)CC3=CC=CC=C3C1. InChi Code: InChI=1S/C18H19NO3S2/c1-3-22-18(21)14-10-12-6-4-5-7-13(12)11-19(14)17(20)15-8-9-16(23-2)24-15/h4-9,14H,3,10-11H2,1-2H3. InChi Key: UIEBLUZPSFAFOC-UHFFFAOYSA-N.