|N-(4-甲氧基苯基)-1-苯基-1H-吡唑-3-胺|CsnPharm

CAS No.: 103141-09-9

FLP 62064 is a potent 5-lipoxygenase (5-LOX) and COX-2 dual inhibitor. FLP 62064 has potently anti-inflammatory activity.

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400-920-2911

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生物活性

描述Prostaglandins (PGs) from the cyclooxygenase pathway and leukotrienes (LTs) from the lipoxygenase pathway are both mediators of the inflammatory process generated from the same arachidonic acid (AA) cascade^[1]. FLP 62064 is a dual inhibitor of prostaglandin synthetase and 5-lipoxygenase with IC₅₀s of 3.6 and 3.1 μM, respectively. In vivo, FPL 62064 inhibited all three parameters with the following order of potency: PGE₂ (prostaglandin E₂)>LTC₄ (leukotriene C₄)>oedema, corresponding to ID₅₀ values of 3.7, 28.3 and 40.8 μg of FPL 62064 per ear, respectively. Furthermore, FPL 62064 (1, 3, 10 μg/site) inhibited production of all three metabolites in a dose-dependent manner. The increase in plasma protein extravasation observed 2 hr after injection of arachidonic acid (range 22-64 μl plasma/site, n = 10) was also dose dependently inhibited by FPL 62064. Moreover, FPL 62064 (250-1000 μg per ear) dose-dependently inhibited oedema, PMN (polymorphonuclear granulocytes) infiltration and the proliferative response to TPA (12-O-tetradecanoylphorbol 13-acetate). In guinea-pigs, FPL 62064 applied topically to irradiated skin produced dose-related inhibition of PGE₂ formation with an IC₅₀ of 11 μg^[2].
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实验方案

技术信息

CAS号

103141-09-9

储存条件

分子式

C16H15N3O

运输

蓝冰

分子量

265.31

别名

溶解度

动物实验配方

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