Nateglinide (Senaglinide, DJN-608, A-4166) is an oral hypoglycaemic agent and non-sulphonylurea insulin secretagogue and DPP IV inhibitor, also is a MRGPRX4 agonist. Nateglinide (Senaglinide, DJN-608, A-4166) stimulated insulin secretion from rat freshly isolated pancreatic islets at concentrations from 3-300 uM in the presence of 2.8 uM glucose. Nateglinide (Senaglinide, DJN-608, A-4166) displaced [3H]-glibenclamide bound to intact HIT-T15 cells in a concentration-dependent manner with Ki of 434 nM. Nateglinide (Senaglinide, DJN-608, A-4166) (1-10 mg/kg, oral) showed a dose-dependent hypoglycaemic effect in fasted beagle dogs.
