FPL 62064
产品说明书
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同义名 : | - |
| CAS号 : | 103141-09-9 | |
| 货号 : | A268943 | |
| 分子式 : | C16H15N3O | |
| 纯度 : | 99%+ | |
| 分子量 : | 265.31 | |
| MDL号 : | MFCD00877802 | |
| 存储条件： |
Pure form Keep in dark place, sealed in dry, room temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 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]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.77mL 0.75mL 0.38mL |
18.85mL 3.77mL 1.88mL |
37.69mL 7.54mL 3.77mL |
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