FPL 62064

FPL 62064 is a potent 5-lipoxygenase (5-LOX) and COX dual inhibitor, with IC₅₀ values of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and prostaglandin synthetase (cyclooxygenase), respectively. FPL 62064 has potent anti-inflammatory activity^[1][2]. IC50 & Target: IC50: 3.5 μM (RBL-1 cytosolic 5-1ipoxygenase), and 3.1 μM (prostaglandin synthetase)^[1] In Vitro: 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^[1]. In Vivo: FPL 62064 (5-20 mg/kg; intraperitoneal injection; female LACA mice) treatment inhibits peritoneal inflammation induced by immune-complex^[1].