| Description: |
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]. |
| Target: |
IC50: 3.5 μM (RBL-1 cytosolic 5-1ipoxygenase), and 3.1 μM (prostaglandin synthetase)[1] |
| In Vivo: |
FPL 62064 (5-20 mg/kg; intraperitoneal injection; female LACA mice) treatment inhibits peritoneal inflammation induced by immune-complex[1]. Animal Model: Female LACA mice (20-30 g) injected with immune complex[1]. 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. |
| 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]. |
| References: |
[1]. Blackham A, et al. FPL 62064, a topically active 5-lipoxygenase/cyclooxygenase inhibitor. Agents Actions. 1990 Jun;30(3-4):432-42.
[2]. Shabaan MA, et al. Synthesis and biological evaluation of pyrazolone analogues as potential anti-inflammatory agents targeting cyclooxygenases and 5-lipoxygenase. Arch Pharm (Weinheim). 2020 Feb 7:e1900308. |
