| 货号 | 11574-50mg |
| 描述 | Inhibiting renal glucose reabsorbtion through the sodium-glucose cotransporter (SGLT) offers an insulin-independent alternative to controlling blood glucose concentrations in patients with type 2 diabetes.1,2 While the majority of glucose is reabsorbed from glomerular filtrate by SGLT2, which is predominantly expressed in the kidney S1 segment of the proximal tubule, SGLT1 reabsorbs glucose in the distal S3 segment of the renal proximal tubule as well as from the small intestine. Dapagliflozin is a first generation, selective SGLT inhibitor that blocks glucose transport with about 100-fold selectivity for SGLT2 (Ki = 6 nM; EC50 = 1.1 nM) over SGLT1 (Ki = 390 nM).3 After single oral doses ranging from 0.1 to 1.0 mg/kg, dapagliflozin increases urinary glucose excretion in both normal and diabetic rats, improves glucose tolerance in normal rats, and reduces hyperglycemia in Zucker diabetic fatty rats.4 Within two weeks of treating diabetic rats with 0.1 to 1.0 mg/kg dapagliflozin, fasting and fed glucose levels have been shown to be significantly lowered as a result of increased glucose utilization accompanied by reduced glucose production.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Tahrani, A.A. and Barnett, A.H. Dapagliflozin: A sodium glucose cotransporter 2 inhibitor in development for type 2 diabetes. Diabetes Ther. 1(2), 45-56 (2010). 2.Komoroski, B.,Vachharajani, N.,Feng, Y., et al. Dapagliflozin, a novel, selective SGLT2 inhibitor, improved glycemic control over 2 weeks in patients with type 2 diabetes mellitus. Clinical Pharmacology and Therapeutics 85(5), 513-519 (2009). 3.Chao, E.C. and Henry, R.R. SGLT2 inhibition - A novel strategy for diabetes treatment. Nature Reviews.Drug Discovery 9(7), 551-559 (2010). 4.Han, S.,Hagan, D.L.,Taylor, J.R., et al. Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic rats. Diabetes 57(6), 1723-1729 (2008). | |
| 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 | 408.9 |
| 分子式 | C21H25ClO6 |
| CAS号 | 461432-26-8 |
| 稳定性 | ≥ 2 years |
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