Teneligliptin is a dipeptidyl peptidase 4 (DPP-4) inhibitor (ICs = 0.37 and 0.29 nM for the human and rat enzymes, respectively). It is selective for DPP-4 over DPP-8 and DPP-9 (ICs = 260 and 540 nM, respectively, for the human enzymes). Teneligliptin (0.03-1 mg/kg) inhibits increases in plasma glucose levels in an oral glucose tolerance test in Zucker fatty rats. It reduces body weight, inhibits hepatic steatosis, and decreases plasma insulin levels in a mouse model of high-fat diet-induced obesity when administered at doses of 30 and 60 mg/kg. Teneligliptin scavenges hydroxyl radicals in a cell-free assay (IC = 0.315 mM) and decreases urinary levels of 8-hydroxy-2′-deoxyguanosine (8-OHdG; ), a marker of oxidative stress, in a DPP-4-deficient rat model of diabetes induced by streptozotocin (STZ; ) when administered at a dose of 10 mg/kg per day.