货号 | 16805-1mg |
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 sulfone is an oxidized metabolite of sulindac that is produced in many mammals but minimally in mice and rats.2,3 It is generally considered to be inactive against COX enzymes, although it can reduce azoxymethane-induced colon cancer in rats.4,5 Sulindac sulfone inhibits aldose reductase (IC50 = 367 nM) in vitro and may contribute to the beneficial pharmacological effects of sulindac on type 2 diabetic complications.6 |
别名 | Exisulind; |
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.Babbar, N.,Ignatenko, N.A.,Casero, R.A., Jr., et al. Cyclooxygenase-independent induction of apoptosis by sulindac sulfone is mediated by polyamines in colon cancer. The Journal of Biological Chemisty 278(48), 47762-47775 (2003). 5.Piazza, G.A.,Alberts, D.S.,Hixson, L.J., et al. Sulindac sulfone inhibits azoxymethane-induced colon carcinogenesis in rats without reducing prostaglandin levels. Cancer Research 57(14), 2909-2915 (1997). 6.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). | |
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 | 372.4 |
分子式 | C20H17FO4S |
CAS号 | 59864-04-9 |
稳定性 | ≥ 2 years |
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