Vildagliptin-d7

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 (K_i = 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)