CAY10686
货号：
9001962-10mg 基本售价：
6608.0 元 规格：
10 mg
产品信息
概述| 货号 | 9001962-10mg |
| 描述 | Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH2 (Item No. 17020) into the biologically active PGE2 (Item No. 14010).1 Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α.2 CAY10686 is a selective 3-aminocarbazole inhibitor of mPGES-1, blocking the synthesis of PGE2 but not PGF2α (Item No. 16010) in A549 cells stimulated with IL-1β (IC50s = 2.9 and >100 µM, respectively).3 It reduces inflammatory pain (acetic acid-induced writhing) in mice by 74% when given intraperitoneally at 10 mg/kg.3 CAY10686 is absorbed through enterocytes, is metabolically stable in human and rat microsome preparations, and is bioavailable in vivo.3 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Jakobsson, P.J.,Thorén, S.,Morgenstern, R., et al. Identification of human prostaglandin E synthase: A microsomal, glutathione-dependent, inducible enzyme, constituting a potential novel drug target. Proceedings of the National Academy of Sciences of the United States of America 96, 7220-7225 (1999).
2.Stichtenoth, D.O.,Thorén, S.,Bian, H., et al. Microsomal prostaglandin E synthase is regulated by proinflammatory cytokines and glucocorticoids in primary rheumatoid synovial cells. Journal of Immunology 167, 469-474 (2001).
3.Alisi, M.A.,Cazzolla, N.,Coletta, I., et al. 3-Aminocarbazole compound, pharmaceutical composition containing it and preparation method therefor. PCT/EP2009/055652, 1-38 (2009).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 398.4 |
| 分子式 | C22H17F3N2O2 |
| CAS号 | 1195786-61-8 |
| 稳定性 | ≥ 2 years |
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