MBX-2982

MBX-2982 is an agonist of GPR119. It reduces nuclear and total protein levels of sterol regulatory element binding protein 1 (SREBP-1) in HepG2 cells and rat primary hepatocytes under high-glucose and -insulin conditions and increases phosphorylation of the inhibitory form, SREBP-1c. MBX-2982 (10 mg/kg) inhibits hepatic lipid accumulation in wild-type, but not GPR119 knockout, mice fed a high-fat diet. It also increases plasma levels of glucagon-like peptide 1 (GLP-1, Cay-24460) in mice when administered at a dose of 10 mg/kg prior to, and to a greater extent following, glucose administration. MBX-2982 increases glucokinase activity in an enzyme assay with an EC50 value of 45.11 µM.Formal Name: 5-ethyl-2-[4-[4-[[4-(1H-tetrazol-1-yl)phenoxy]methyl]-2-thiazolyl]-1-piperidinyl]-pyrimidine. CAS Number: 1037792-44-1. Molecular Formula: C22H24N8OS. Formula Weight: 448.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: Chloroform: 30 mg/ml. lambdamax: 250 nm. SMILES: CCC1=CN=C(N2CCC(C3=NC(COC4=CC=C(N5N=NN=C5)C=C4)=CS3)CC2)N=C1. InChi Code: InChI=1S/C22H24N8OS/c1-2-16-11-23-22(24-12-16)29-9-7-17(8-10-29)21-26-18(14-32-21)13-31-20-5-3-19(4-6-20)30-15-25-27-28-30/h3-6,11-12,14-15,17H,2,7-10,13H2,1H3. InChi Key: NFTMKHWBOINJGM-UHFFFAOYSA-N.