产品描述:
V-0219 is a positive allosteric modulator (PAM) of the glucagon-like peptide 1 receptor (GLP-1R).{67722} It is selective for GLP-1R over a panel of 54 other receptors, ion channels, and transporters at 10 µM. V-0219 (0.001-1 nM) potentiates GLP-1-induced cAMP accumulation in HEK293 cells expressing human GLP-1R. It also potentiates GLP-1-induced insulin secretion in INS-1E rat insulinoma cells, an effect that can be blocked by the GLP-1R antagonist exendin (9-39) amide. V-0219 improves glucose tolerance in wild-type, but not Glp1r knockout, mice when administered at a dose of 0.1 mg/kg and enhances a reduction in food intake induced by the GLP-1R agonist exendin-4 in rats at 0.001 mg/kg.