YS-121
货号：
13665-25mg 基本售价：
10542.0 元 规格：
25 mg
产品信息
概述| 货号 | 13665-25mg |
| 描述 | Microsomal prostaglandin E2 synthase-1 (mPGES-1), with cyclooxygenase-2 (COX-2), synthesizes PGE2, which is directly involved in signaling during inflammation, fever, and pain. 5-Lipoxygenase (5-LO) initiates the synthesis of leukotrienes (LTs), which are pro-inflammatory mediators. YS-121 is a dual inhibitor of mPGES-1 (IC50 = 3.9 μM)1 and 5-LO (IC50 = 4.1 μM).2 It effectively inhibits PGE2 and LT synthesis in both cell free and intact cell assays. Moreover, YS-121 (1.5 mg/kg, intraperitoneal) reduced pleural levels of PGE2 and LTB4 while blocking exudate formation and leukocyte infiltration in carrageenan-induced rat pleurisy.3 YS-121 has minor effects on COX-1 and COX-2, inhibiting these enzymes 24.8% and 38%, respectively, at 10 μM.1 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Koeberle, A.,Zettl, H.,Greiner, C., et al. Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase. Journal of Medicinal Chemistry 51, 8068-8076 (2008).
2.Werz, O.,Greiner, C.,Koeberle, A., et al. Novel and potent inhibitors of 5-lipoxygenase product synthesis based on the structures of pirinixic acid. Journal of Medicinal Chemistry 51, 5449-5453 (2008).
3.Koeberle, A.,Rossi, A.,Zettl, H., et al. The molecular pharmacology and in vivo activity of 2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)octanoic acid (YS121), a dual inhibitor of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase. Journal of Pharmacology and Experimental Therapeutics 332, 840-848 (2010).
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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 | 408 |
| 分子式 | C20H26ClN3O2S |
| CAS号 | 916482-17-2 |
| 稳定性 | ≥ 1 year |
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