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; ) 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.
