FPL 62064

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

FPL 62064 是一种有效的 5-脂氧合酶 (5-LOX) 和 COX 双重抑制剂（RBL-1 胞质 5-脂氧合酶和前列腺素合成酶的 IC50 分别为 3.5 μM 和 3.1 μM）。

FPL 62064 is a potent ?dual inhibitor of 5-lipoxygenase (5-LOX) and COX (IC50 of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and prostaglandin synthetase respectively).?

FPL 62064 inhibits both 5-1ipoxygenase (IC50 of 3.5 μM for RBL-1 cytosolic 5-1ipoxygenase) and prostaglandin synthetase (IC50 of 3.1 μM for seminal vesicle prostaglandin synthetase ) with equal facility in the isolated enzyme screens. However in the intact RBL-I cell prostaglandin synthetase (IC50 of 3.6 μM) is more readily inhibited by FPL 62064 than is 5-1ipoxygenase (IC50 of 31 μM). This difference in sensitivity is not reflected in the mouse macrophage where the IC50s for leukotriene (IC50 of 0.72 μM) and prostaglandin (IC50 of 0.43 μM) production are similar.

FPL 62064 (5-20 mg/kg; intraperitoneal injection; female LACA mice) treatment inhibits peritoneal inflammation induced by immune-complex. Animal Model:Female LACA mice (20-30 g) injected with immune complex.Dosage:5 mg/kg, 10 mg/kg, 20 mg/kg Administration:Intraperitoneal injection Result:Produced a dose-related inhibition of dye extravasation, leukotriene C4 (LTC4) and prostaglandin E2 (PGE2) formation.

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Chromatin/Epigenetic

COX

COX|5-LOX

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103141-09-9

265.31

C16H15N3O

>98% (HPLC)

DMSO:250 mg/mL (942.29 mM; Need ultrasonic)

COc1ccc(Nc2ccn(n2)-c2ccccc2)cc1

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(-20℃)

With Ice Pack

≥ 2 years