| 货号 | 21507-1mg |
| 描述 | Ertugliflozin potently inhibits the sodium-glucose cotransporter 2 (SGLT2), increasing the excretion of glucose with a 2,000-fold selectivity over SGLT1 (IC50 = 0.877 and 1,960 nM, respectively, for human isoforms in vitro).1 Inhibiting renal glucose reabsorption in this way offers an insulin-independent alternative to controlling blood glucose concentrations in patients with type 2 diabetes mellitus.2,3 In Phase III clinical trials at doses of 5 and 15 mg, ertugliflozin reduced plasma glucose and HbA1c levels as well as decreased body weight.4,5 |
| 别名 | PF-04971729; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Mascitti, V.,Maurer, T.S.,Robinson, R.P., et al. Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors. J. Med. Chem. 54(8), 2952-2960 (2011). 2.Tahrani, A.A.,Bailey, C.J.,Del Prato, S., et al. Management of type 2 diabetes: New and future developements in treatment. New Horizons 6736(11), 60207-60209 (2011). 3.Kalgutkar, A.S.,Tugnait, M.,Zhu, T., et al. Preclinical species and human disposition of PF-04971729, a selective inhibitor of the sodium-dependent glucose cotransporter 2 and clinical candidate for the treatment of type 2 diabetes mellitus. Drug Metab. Dispos. 39(9), 1609-1619 (2011). 4.Terra, S.G.,Focht, K.,Davies, M., et al. Phase III, efficacy and safety study of ertugliflozin monotherapy in people with type 2 diabetes mellitus inadequately controlled with diet and exercise alone. Diabetes Obes. Metab. 19(5), 721-728 (2017). 5.Amin, N.B.,Wang, X.,Jain, S.M., et al. Dose-ranging efficacy and safety study of ertugliflozin, a sodium-glucose co-transporter 2 inhibitor, in patients with type 2 diabetes on a background of metformin. Diabetes Obes. Metab. 17(6), 591-598 (2015). | |
| 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 | 436.9 |
| 分子式 | C22H25ClO7 |
| CAS号 | 1210344-57-2 |
| 稳定性 | ≥ 2 years |
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