| 货号 | 13217-1mg |
| 描述 | Microsomal prostaglandin E2 synthase-1 (mPGES-1) is the terminal enzyme in the biosynthesis of PGE2.1,2,3 MF63 is a potent, selective, and orally active inhibitor of human mPGES-1 (IC50 = 1.3 nM).4,5 It displays greater than 1,000-fold selectivity over other prostanoid synthases.5 MF63 also potently inhibits guinea pig mPGES-1 (IC50 = 0.9 nM) but not mouse or rat mPGES-1.5 In guinea pigs or in mice expressing human mPGES-1, MF63 prevents LPS-induced pyresis, hyperalgesia, and iodoacetate-induced osteoarthritic pain.5 It does not produce the gastrointestinal toxicity that is caused by non-selective COX inhibitors, although it markedly suppresses PGE2 synthesis in the stomach.5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Samey, A.V.,Monrad, S., and Crofford, L.J. Microsomal prostaglandin E synthase-1: The inducible synthase for prostaglandin E2. Arthritis Research & Therapy 7(3), 114-117 (2005). 2.Friesen, R.W., and Mancini, J.A. Microsomal prostaglandin E2 synthase-1 (mPGES-1): A novel anti-inflammatory therapeutic target. Journal of Medicinal Chemistry 51(14), 4059-4067 (2008). 3.Hara, S.,Kamei, D.,Sasaki, Y., et al. Prostaglandin E synthases: Understanding their pathophysiological roles through mouse genetic models. Biochimie 92, 651-659 (2010). 4.Côté, B.,Boulet, L.,Brideau, C., et al. Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. Bioorganic & Medicinal Chemistry Letters 17, 6816-6820 (2007). 5.Xu, D.,Rowland, S.E.,Clark, P., et al. MF63 [2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-isophthalonitrile], a selective microsomal prostaglandin E synthase-1 inhibitor, relieves pyresis and pain in preclinical models of inflammation. Journal of Pharmacology and Experimental Therapeutics 326(3), 754-763 (2008). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | 22 |
| 纯度 | ≥98% |
| 计算分子量 | 378.8 |
| 分子式 | C23H11ClN4 |
| CAS号 | 892549-43-8 |
| 稳定性 | ≥ 2 years |
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