| 货号 | 10004387-5mg |
| 描述 | Sulindac (Item No. 10004386) is a non-steroidal anti-inflammatory drug that has an extensive epidemiology documenting reduced human colorectal cancer. In mouse models, sulindac was found not only to inhibit the enzymatic activity of polyp-associated COX-2, but also to downregulate the expression of colonic COX-2 protein to control levels.1 Sulindac sulfide is a metabolite of sulindac that has diverse activities.2,3 It inhibits both COX-1 and COX-2 (IC50s = 1.9 and 1.21 µM, respectively), whereas the parent compound, sulindac, is much less effective (IC50 = 58 µM for COX-2 and > 100 µM for COX-1).4 Sulindac sulfide also inhibits aldose reductase (IC50 = 279 nM), blocking NADPH-dependent reduction of glucose to sorbitol, and reducing type 2 diabetic complications.5 It increases the expression and activity of NAD(P)H quinone oxidoreductase 1.6 Sulindac sulfide inhibits colorectal cancer growth both in vitroandin vivo.7 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Boolbol, S.K.,Dannenberg, A.J.,Chadburn, A., et al. Cyclooxygenase-2 overexpression and tumor formation are blocked by sulindac in a murine model of familial adenomatous polyposis. Cancer Research 56, 2556-2560 (1996). 2.Kitamura, S., and Tatsumi, K. In vitro metabolism of sulindac and sulindac sulfide: Enzymatic formation of sulfoxide and sulfone. Japanese Journal of Pharmacology 32(5), 833-838 (1982). 3.Brunell, D.,Sagher, D.,Kesaraju, S., et al. Studies on the metabolism and biological activity of the epimers of sulindac. Drug Metabolism and Disposition 39(6), 1014-1021 (2011). 4.Warner, T.D.,Giuliano, F.,Vojnovic, I., et al. Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: A full in vitro analysis. Proceedings of the National Academy of Sciences of the United States of America 96(13), 7563-7568 (1999). 5.Zheng, X.,Zhang, L.,Zhai, J., et al. The molecular basis for inhibition of sulindac and its metabolites towards human aldose reductase. FEBS Letters 586(1), 55-59 (2012). 6.Kung, H.N.,Weng, T.Y.,Liu, Y.L., et al. Sulindac compounds facilitate the cytotoxicity of β-lapachone by up-regulation of NAD(P)H quinone oxidoreductase in human lung cancer cells. PLoS One 9(2), 1-15 (2014). 7.Williams, C.S.,Goldman, A.P.,Sheng, H., et al. Sulindac sulfide, but not sulindac sulfone, inhibits colorectal cancer growth. Neoplasia 1(2), 170-176 (1999). | |
| 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 | 340.4 |
| 分子式 | C20H17FO2S |
| CAS号 | 49627-27-2 |
| 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。 |