A positive allosteric modulator of GLP-1R (EC50 = 0.66 µM in a reporter assay), selective for GLP-1R over GLP-2R, as well as glucose-dependent insulinotropic polypeptide, glucagon, and the parathyroid hormone receptors, induces cAMP accumulation and intracellular calcium mobilization in CHO cells expressing human GLP-1R (EC50s = 5 and 6.3 µM, respectively), increases glucose-induced insulin secretion in pancreatic islets isolated from patients with type 2 diabetes at 3 and 10 µM, increases plasma insulin levels in an intravenous glucose tolerance test in rats at 10 mg/kg
