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。
| 生物活性 | Pyrrophenone is a potent and specific cytosolicphospholipase A2α (cPLA2α) inhibitor with an IC50value of 4.2 nM[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | Pyrrophenone shows potent inhibition of arachidonic acid release, prostaglandin E2, thromboxane B2, and leukotriene B4formation in human whole blood[1].
Pyrrophenone inhibits the production of arachidonic acid (AA) (IC50=24±1.7 nM), PGE2(IC50=25±19 nM),, and LTC4(IC50=14±6.7 nM),from THP-1 cells stimulated with A23187[1].
Pyrrophenone inhibits the production of AA (IC50=0.19±0.068 μM), PGE2(IC50=0.20±0.047 μM), TXB2(IC50=0.16±0.093 μM),and LTB4(IC50=0.32±0.24 μM) from human whole blood stimulated with A23187[1].
Pyrrophenone (0.1-0.5 μM, 48 h) inhibits the growth of PC-PTC3 and PCCl3cells[2].
Cell Proliferation Assay[2] | Cell Line: | PC-PTC3 and PCCl3cells | | Concentration: | 0.1, 0.3, and 0.5 μM | | Incubation Time: | 48 hours | | Result: | Significantly inhibited basal PC-PTC3 cell proliferation at concentrations as low as 0.1 μM.
Basal cell proliferation of normal PCCl3cells was also inhibited by 0.5 μM, although to a lesser extent. |
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体内研究
(In Vivo) | Pyrrophenone (administered i.p. at 20 mg/kg 30 min before LPS injection.) suppresses bronchoalveolar lavage (BAL) levels of leukotriene B4 (LTB4) and platelet activating factor (PAF)[3].
| Animal Model: | Specific pathogen-free female BALB/c mice[3] | | Dosage: | 20 mg/kg | | Administration: | Administered i.p. 30 min before LPS injection | | Result: | Suppressed the recruitment of neutrophils and eosinophils, but not macrophages. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(117.65 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.1765 mL | 5.8826 mL | 11.7653 mL | | 5 mM | 0.2353 mL | 1.1765 mL | 2.3531 mL | | 10 mM | 0.1177 mL | 0.5883 mL | 1.1765 mL |
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