| 货号 | 18267-50mg |
| 描述 | LY315920 is an inhibitor of human group IIA (hGIIA) secretory phospholipase A2(sPLA2; IC50 = 9 nM).1 It also potently inhibits human GIIE and GX isoforms, as well as the corresponding mouse isoforms, but poorly inhibits other PLA2enzymes.1,2,3,4 LY315920 inhibits sPLA2-induced release of thromboxane A2 from isolated guinea pig lung bronchoalveolar lavage cells (IC50 = 0.79 µM).2 Intravenous or oral administration of LY315920 to transgenic mice expressing human sPLA2 inhibits serum sPLA2 activity in a dose-related manner over four hours.2 |
| 别名 | Varespladib; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Draheim, S.E.,Bach, N.J.,Dillard, R.D., et al. Indole inhibitors of human nonpancreatic secretory phospholipase A2. 3. Indole-3-glyoxamides. Journal of Medicinal Chemistry 39, 5159-5175 (1996). 2.Snyder, D.W.,Bach, N.J.,Dillard, R.D., et al. Pharmacology of LY315920/S-5920, [[3-(aminooxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy] acetate, a potent and selective secretory phospholipase A2 inhibitor: A new class of anti-inflammatory drugs, SPI. Journal of Pharmacology and Experimental Therapeutics 288(3), 1117-1124 (1999). 3.Oslund, R.C.,Cermak, N. and Gelb, M.H. Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. Journal of Medicinal Chemistry 51(15), 4708-4714 (2008). 4.Smart, B.P.,Pan, Y.H.,Weeks, A.K., et al. Inhibition of the complete set of mammalian secreted phospholipases A2 by indole analogues: A structure-guided study. Bioorganic & Medicinal Chemistry 12, 1737-1749 (2004). | |
| 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 | 380.4 |
| 分子式 | C21H20N2O5 |
| CAS号 | 172732-68-2 |
| 稳定性 | ≥ 2 years |
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