CAY10678
货号：
15129-10mg 基本售价：
6608.0 元 规格：
10 mg
产品信息
概述| 货号 | 15129-10mg |
| 描述 | Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH2 into the biologically active PGE2.1 Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α.2 CAY10678 is a benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC50 = 0.09 and 0.9 µM, respectively).3 It has minimal effects on COX-1, COX-2, PGIS, and hematopoietic PGDS at 50 μM but reduces lipocalin-type PGDS activity by 60% at this concentration.3 CAY10678 dose-dependently blocks PGE2 synthesis in isolated cells and whole blood treated with LPS or IL-1β.3 It also dose-dependently reduces PGE2 synthesis and cell recruitment during inflammation in mice.3 |
| 别名 | mPGES-1 Inhibitor III; |
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.Leclerc, P.,Idborg, H.,Spahiu, L., et al. Characterization of a human and murine mPGES-1 inhibitor and comparison to mPGES-1 genetic deletion in mouse models of inflammation. Prostaglandins & Other Lipid Mediators 107, 26-34 (2013).
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| 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 | 382.5 |
| 分子式 | C23H34N4O |
| CAS号 | 1268709-57-4 |
| 稳定性 | ≥ 2 years |
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