| 货号 | 13252-50mg |
| 描述 | Dipeptidyl peptidase 4 (DPP-4) is an intrinsic membrane glycoprotein that acts as an exopeptidase, cleaving oligopeptides after the second amino acid from the N-terminal end.1 One of its substrates is glucagon-like peptide 1, an incretin that stimulates insulin biosynthesis and secretion while inhibiting glucagon release in a glucose-dependent manner.1,2 Sitagliptin is a potent inhibitor of DPP-4 (IC50 = 18 nM).2 It only modestly inhibits DPP-8 (IC50 = 48 µM) and is without effect on several related peptidases, including DPP-9, DPP-II, and amino peptidase P.2,3 Sitagliptin is orally active, rapidly absorbed, and inhibits DPP-4 in plasma.1 It lowers fasting plasma glucose, glycosylated hemoglobin, and two-hour postprandial glucose levels in patients with type 2 diabetes.4 In addition to having use in type 2 diabetes, gliptins, including sitagliptin, have positive cardiovascular and anti-inflammatory effects.1,4,5 |
| 别名 | INN;MK-431;ONO-5435; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Ahrén, B. DPP-4 inhibitors. Best Pract.Res.Clin.Endocrinol.Metab. 21(4), 517-533 (2007). 2.Biftu, T.,Feng, D.,Qian, X., et al. (3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Bioorganic & Medicinal Chemistry Letters 17(1), 49-52 (2007). 3.Kim, D.,Kowalchick, J.E.,Edmondson, S.D., et al. Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: Close analogs of JANUVIAT (sitagliptin phosphate). Bioorganic & Medicinal Chemistry Letters 17(12), 3373-3377 (2007). 4.Pham, D.Q.,Nogid, A. and Plakogiannis, R. Sitagliptin: A novel agent for the management of type 2 diabetes mellitus. American Journal of Health-System Pharmacy 65, 521-531 (2008). 5.Scheen, A.J. Cardiovascular effects of gliptins. Nat.Rev.Cardiol. 10(2), 73-84 (2013). | |
| 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 | 505.3 |
| 分子式 | C16H15F6N5O • H3PO4 |
| CAS号 | 654671-78-0 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |