Vildagliptin-d7 has 7 deuteriums. Vildagliptin-d7 is intended for use as an internal standard for the quantification of vildagliptin by GC- or LC-MS. Vildagliptin is an inhibitor of DPP-4 (IC50 = 3.5-34 nM).1,2 It also inhibits DPP-8 and DPP-9 (Ki = 810 and 95 nM, respectively) but not DPP-2 or the related fibroblast activation protein α.3 Through its effects on DPP-4, it blocks the degradation of several circulating peptides, including incretins (stimulators of insulin secretion) like glucose-dependent insulinotropic polypeptide and glucagon-like peptide-1.4,5 Vildagliptin reduces fasting and postprandial glucose levels and decreases inflammatory and oxidative stress in diverse animal models of disease.6,7
1.Weber, A.E.Dipeptidyl peptidase IV inhibitors for the treatment of diabetesJournal of Medicinal Chemistry47(17)4135-4141(2004) 2.Parmee, E.R., He, J., Mastracchio, A., et al.4-amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitorsBioorganic & Medicinal Chemistry Letters14(1)43-46(2004) 3.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) inhibitorsBioorganic & Medicinal Chemistry20(19)5864-5883(2012) 4.Mari, A., Sallas, W.M., He, Y.L., et al.Vildagliptin, a dipeptidyl peptidase-IV inhibitor, improves model-assessed β-cell function in patients with type 2 diabetesJournal of Clinical Endocrinology and Metabolism90(8)4888-4894(2005) 5.Burkey, B.F., Li, X., Bolognese, L., et al.Acute and chronic effects of the incretin enhancer vildagliptin in insulin-resistant ratsJournal of Pharmacology and Experimental Therapeutics315(2)688-695(2005) 6.Scheen, A.J.Cardiovascular effects of gliptinsNat.Rev.Cardiol.10(2)73-84(2013) 7.Strain, W.D., Lukashevich, V., Kothny, W., et al.Individualised treatment targets for elderly patients with type 2 diabetes using vildagliptin add-on or lone therapy (INTERVAL): A 24 week, randomised, double-blind, placebo-controlled studyLangmuir382(9890)409-416(2013)