| 货号 | 14705-10mg |
| 描述 | Glyptins are a class of oral antihyperglycemic agents that inhibit dipeptidyl peptidase 4 (DPP-4), which can act as a serine exopeptidase.1 In addition to having use in type 2 diabetes, gliptins have positive cardiovascular and anti-inflammtatory effects.1,2,3 Vildagliptin is an inhibitor of DPP-4 (IC50 = 3.5-34 nM).4,5 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.6 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-1.7,8 Vildagliptin reduces fasting and postprandial glucose levels and decreases inflammatory and oxidative stress in diverse animal models of disease.1,3 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Scheen, A.J. Cardiovascular effects of gliptins. Nat.Rev.Cardiol. 10(2), 73-84 (2013). 2.Doupis, J. and Veves, A. DPP4 inhibitors: A new approach in diabetes treatment. Advances in Therapy 25(7), 627-643 (2008). 3.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 study. Langmuir 382(9890), 409-416 (2013). 4.Weber, A.E. Dipeptidyl peptidase IV inhibitors for the treatment of diabetes. Journal of Medicinal Chemistry 47(17), 4135-4141 (2004). 5.Parmee, E.R.,He, J.,Mastracchio, A., et al. 4-amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors. Bioorganic & Medicinal Chemistry Letters 14(1), 43-46 (2004). 6.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) inhibitors. Bioorganic & Medicinal Chemistry 20(19), 5864-5883 (2012). 7.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 diabetes. Journal of Clinical Endocrinology and Metabolism 90(8), 4888-4894 (2005). 8.Burkey, B.F.,Li, X.,Bolognese, L., et al. Acute and chronic effects of the incretin enhancer vildagliptin in insulin-resistant rats. Journal of Pharmacology and Experimental Therapeutics 315(2), 688-695 (2005). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 303.4 |
| 分子式 | C17H25N3O2 |
| CAS号 | 274901-16-5 |
| 稳定性 | ≥ 2 years |
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