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 Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(942.29 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
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