Pyrrophenone 是一种有效且特异性的胞质磷脂酶 A2α (cPLA2α) 抑制剂，IC50 值为 4.2 nM。
| Cas No. | 341973-06-6 |
| Canonical SMILES | FC(C=C1F)=CC=C1C(C2=CC=CC=C2C(N3[C@H](CNC(C4=CC=C(/C=C5C(NC(S\5)=O)=O)C=C4)=O)C[C@@H](SC(C6=CC=CC=C6)(C7=CC=CC=C7)C8=CC=CC=C8)C3)=O)=O |
| 分子式 | C49H37F2N3O5S2 |
| 分子量 | 850 |
| 溶解度 | DMF: 12.5 mg/ml,DMSO: 15 mg/ml,DMSO:PBS (pH 7.2) (1:10): 0.1 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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). 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). Its action is reversible and selective, as pyrrophenone inhibits the secretory type IB and IIA PLA2s with more than a hundred-fold less potency. Pyrrophenone has also been shown to inhibit calcium ionophore (A23187)-stimulated AA release from monocytic cells, interleukin-1-induced PGE2 synthesis in mesangial cells, and the production of PGE2, LTs, and platelet-activating factor by human neutrophils, always with maximal inhibition at concentrations below 1 μM. |
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