| 货号 | 13294-10mg |
| 描述 | The group IVA phospholipase A2(PLA2), known as calcium-dependent cytosolic PLA2(cPLA2), selectively releases arachidonic acid (AA) from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins (PGs) and leukotrienes (LTs).1,2 Pyrrophenone inhibits cPLA2α with an IC50 of 4.2 nM in enzyme assays and potently blocks the release of AA and the production of PGE2 and LTC4 in cells (IC50 = 24, 25, and 14 nM, respectively).3 Its action is reversible and selective, as pyrrophenone inhibits the secretory type IB and IIA PLA2s with more than a hundred-fold less potency.4 Pyrrophenone has also been shown to inhibit calcium ionophore (A23187)-stimulated AA release from monocytic cells,4 interleukin-1-induced PGE2 synthesis in mesangial cells,4 and the production of PGE2, LTs, and platelet-activating factor by human neutrophils,5 always with maximal inhibition at concentrations below 1 μM. |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Ghosh, M.,Stewart, A.,Tucker, D.E., et al. Role of cytosolic phospholipase A2 in prostaglandin E2 production by lung fibroblasts. American Journal of Respiration, Cell, and Molecular Biology 30, 91-100 (2004). 2.Liberty, I.F.,Raichel, L.,Hazan-Eitan, Z., et al. Cytosolic phospholipase A2 is responsible for prostaglandin E2 and leukotriene B4 formation in phagocyte-like PLB-985 cells: Studies of differentiated cPLA2-deficient PLB-985 cells. Journal of Leukocyte Biology 76, 176-184 (2004). 3.Seno, K.,Okuno, T.,Nishi, K., et al. Pyrrolidine inhibitors of human cytosolic phospholipase A2 part2: Synthesis of potent and crystallized 4-triphenylmethylthio derivative “pyrrophenone”. Bioorganic & Medicinal Chemistry Letters 11, 587-590 (2001). 4.Ono, T.,Yamada, K.,Chikazawa, Y., et al. Characterization of a novel inhibitor of cytosolic phospholipase A2α, pyrrophenone. Biochemistry Journal 363, 727-735 (2002). 5.Flamand, N.,Picard, S.,Lemieux, L., et al. Effects of pyrrophenone, an inhibitor of group IVA phospholipase A2, on eicosanoid and PAF biosynthesis in human neutrophils. British Journal of Pharmacology 149, 385-392 (2006). | |
| 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 | 850 |
| 分子式 | C49H37F2N3O5S2 |
| CAS号 | 341973-06-6 |
| 稳定性 | ≥ 2 years |
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