FPL 62064

FLP 62064 is a potent 5-lipoxygenase (5-LOX) and COX-2 dual inhibitor. FLP 62064 has potently anti-inflammatory activity.

Product information

CAS Number: 103141-09-9

Molecular Weight: 265.31

Formula: C16H15N3O

Chemical Name: 1H-Pyrazol-3-amine, N-(4-methoxyphenyl)-1-phenyl-

Smiles: COC1C=CC(=CC=1)NC1C=CN(N=1)C1C=CC=CC=1

InChiKey: WKLGNFJHVJIZPK-UHFFFAOYSA-N

InChi: InChI=1S/C16H15N3O/c1-20-15-9-7-13(8-10-15)17-16-11-12-19(18-16)14-5-3-2-4-6-14/h2-12H,1H3,(H,17,18)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

In Vivo:

FPL 62064 (5-20 mg/kg; intraperitoneal injection; female LACA mice) treatment inhibits peritoneal inflammation induced by immune-complex.

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.

Products are for research use only. Not for human use.