FPL 62064

Names

[ Name ]:
FPL 62064

[Synonym ]:
N-(4-Methoxyphenyl)-1-phenyl-1H-pyrazol-3-amine
fd7168
1H-Pyrazol-3-amine, N-(4-methoxyphenyl)-1-phenyl-

Biological Activity

[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].

[Related Catalog]:

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Metabolic Enzyme/Protease >> 5-Lipoxygenase

Signaling Pathways >> Immunology/Inflammation >> COX

[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]. 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.

[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.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
442.6±25.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₆H₁₅N₃O

[ Molecular Weight ]:
265.310

[ Flash Point ]:
221.5±23.2 °C

[ Exact Mass ]:
265.121521

[ PSA ]:
39.08000

[ LogP ]:
3.49

[ Vapour Pressure ]:
0.0±1.1 mmHg at 25°C

[ Index of Refraction ]:
1.610

[ Storage condition ]:
-20°C

Safety Information

[ Hazard Codes ]:
Xi

[ HS Code ]:
2933199090

Customs

[ HS Code ]: 2933199090

[ Summary ]:
2933199090. other compounds containing an unfused pyrazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Related Compounds

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