FPL 62064

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Chemical Structure| 103141-09-9 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

溶解度 : -
动物实验配方:
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.77mL

0.75mL

0.38mL

18.85mL

3.77mL

1.88mL

37.69mL

7.54mL

3.77mL

参考文献

[1]Shabaan MA, Kamal AM, Faggal SI, Elsahar AE, Mohamed KO. Synthesis and biological evaluation of pyrazolone analogues as potential anti-inflammatory agents targeting cyclooxygenases and 5-lipoxygenase. Arch Pharm (Weinheim). 2020;353(4):e1900308

[2]Blackham A, Griffiths RJ, Hallam C, et al. FPL 62064, a topically active 5-lipoxygenase/cyclooxygenase inhibitor. Agents Actions. 1990;30(3-4):432-442