| 货号 | 19888-25mg |
| 描述 | Tolbutamide is an inhibitor of sulfonylurea receptor 1 (SUR1; IC50 = 2 µM) linked to inwardly rectifying potassium channel KIR6.2.1 It does not block SUR2.2 Inhibition of SUR1 and the attendant potassium efflux from β-cells stimulates insulin secretion, which has applications in managing type 2 diabetes.2,3 Tolbutamide is metabolized by the cytochrome P450 (CYP) isoform 2C9 and, to a lesser extent, CYP2C8 and CYP2C19 to 4-hydroxy tolbutamide (Item No. 10008520).4,5 The 4-hydroxylation of tolbutamide is used as a probe reaction for CYP2C9 activity.4 |
| 别名 | D 860;NSC 23813;NSC 87833;U-2043; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Bryan, J., and Aguilar-Bryan, L. Sulfonylurea receptors: ABC transporters that regulate ATP-sensitive K+ channels. Biochim Biophys. Acta. 1461(2), 285-303 (1999). 2.Proks, P.,Reimann, F.,Green, N., et al. Sulfonylurea stimulation of insulin secretion. Diabetes 51(3), S368-S376 (2002). 3.Melander, A. Kinetics-effect relations of insulin-releasing drugs in patients with type 2 diabetes. Diabetes 53, S151-S155 (2004). 4.Yuan, R.,Madani, S.,Wei, X.-X., et al. Evaluation of cytochrome P450 probe substrates commonly used by the pharmaceutical industry to study in vitro drug interactions. Drug Metab. Dispos. 30(12), 1311-1319 (2002). 5.Miners, J.P., and Birkett, D.J. Cytochrome P4502C9: An enzyme of major importance in human drug metabolism. Br. J. Clin. Pharmacol. 45(6), 525-538 (1998). | |
| 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 | 270.3 |
| 分子式 | C12H18N2O3S |
| CAS号 | 64-77-7 |
| 稳定性 | ≥ 2 years |
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