| 货号 | 19141-1mg |
| 描述 | Inhibiting renal glucose reabsorption 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. Sotagliflozin is an orally available L-xyloside that potently inhibits both SGLT1 and SGLT2 (IC50s = 36 and 1.8 nM, respectively, for human isoforms in vitro).3 It improves glycemic control in nonobese diabetes prone mice with type 1 diabetes and in patients with type 2 diabetes in a randomized, placebo-controlled clinical trial.3,4 Sotagliflozin also increases serum glucagon-like peptide 1 and peptide YY levels by reducing SGLT1-mediated absorption of intestinal glucose.5 |
| 别名 | LP 802034;LX4211; |
| 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.Zambrowicz, B.,Freiman, J.,Brown, P.M., et al. LX4211, a dual SGLT1/SGLT2 inhibitor, improved glycemic control in patients with type 2 diabetes in a randomized, placebo-controlled trial. Clinical Pharmacology and Therapeutics 92(2), 158-169 (2012). 4.Powell, D.R.,Doree, D.,Jeter-Jones, S., et al. Sotagliflozin improves glycemic control in nonobese diabetes-prone mice with type 1 diabetes. Diabetes Metab.Syndr.Obes. 8, 121-127 (2015). 5.Powell, D.R.,Smith, M.,Greer, J., et al. LX4211 increases serum glucagon-like peptide 1 and peptide YY levels by reducing sodium/glucose cotransporter 1 (SGLT1)-mediated absorption of intestinal glucose. Journal of Pharmacology and Experimental Therapeutics 345(2), 250-259 (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 | 424.9 |
| 分子式 | C21H25ClO5S |
| CAS号 | 1018899-04-1 |
| 稳定性 | ≥ 2 years |
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