1. Metabolic Enzyme/Protease
    Immunology/Inflammation
  2. Lipoxygenase
    COX
  3. FPL 62064

FPL 62064 

Cat. No.: HY-105024 Purity: 98.46%
Handling Instructions

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.

For research use only. We do not sell to patients.

FPL 62064 Chemical Structure

FPL 62064 Chemical Structure

CAS No. : 103141-09-9

Size Price Stock Quantity
10mM/1ml USD 205 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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].

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.
Molecular Weight

265.31

Formula

C₁₆H₁₅N₃O

CAS No.

103141-09-9

SMILES

COC1=CC=C(NC2=NN(C3=CC=CC=C3)C=C2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Store at room temperature

*In solvent : -80°C, 6 months; -20°C, 1 month (Store at room temperature)

Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7692 mL 18.8459 mL 37.6918 mL
5 mM 0.7538 mL 3.7692 mL 7.5384 mL
10 mM 0.3769 mL 1.8846 mL 3.7692 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.67 mg/mL (6.29 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.67 mg/mL (6.29 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

FPL 62064FPL62064FPL-62064LipoxygenaseCOXLOXCyclooxygenaseProstaglandinsynthetase5-lipoxygenaseanti-inflammatoryCOX-25-LOXInhibitorinhibitorinhibit

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Product Name:
FPL 62064
Cat. No.:
HY-105024
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