Vildagliptin is an inhibitor of dipeptidyl peptidase 4 (DPP-4; Ki = 0.003 ?M).1 It is selective for DPP-4 over DPP-2, DPP-8, and DPP-9 (Kis = >500, 0.81, and 0.095 ?M, respectively). Vildagliptin (3 mg/kg) decreases plasma glucose levels and increases plasma insulin levels during an oral glucose challenge in Zucker fa/fa rats.2 It prevents increases in liver triglyceride and thiobarbituric acid reactive substance (TBARS) levels in a mouse model of non-alcoholic fatty liver disease (NAFLD) induced by a high-cholesterol diet.3 Formulations containing vildagliptin have been used in the treatment of type 2 diabetes.
1.Ikuma, Y., Hochigai, H., Kimura, H., et al.Discovery of 3H-imidazol[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitorsBioorg. Med. Chem.20(19)5864-5883(2012) 2.Burkey, B.F., Li, X., Bolognese, L., et al.Acute and chronic effects of the incretin enhancer vildagliptin in insulin-resistant ratsJ. Pharmacol. Exp. Ther.315(2)688-695(2005) 3.Kamal, S.M.Anti-oxidant and anti-inflammatory effects of vildagliptin in non-alcoholic fatty liver disease of miceInt. J. Med. Nano Res.1(1)1-5(2014)