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FPL 62064

Alias: FPL 62064; FPL-62064
Cat No.:V40032 Purity: ≥98%
FPL 62064 is a potent dual (bifunctional) inhibitor of 5-lipoxygenase (5-LOX) and COX, with IC50s for RBL-1 cytosolic 5-lipoxygenase and prostaglandin synthase (cyclooxygenase).
FPL 62064
FPL 62064 Chemical Structure CAS No.: 103141-09-9
Product category: New2
This product is for research use only, not for human use. We do not sell to patients.
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5mg
10mg
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Product Description
FPL 62064 is a potent dual (bifunctional) inhibitor of 5-lipoxygenase (5-LOX) and COX, with IC50s for RBL-1 cytosolic 5-lipoxygenase and prostaglandin synthase (cyclooxygenase). 3.5 μM and 3.1 μM respectively. FPL 62064 has potent anti~inflammatory activity.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
In the separase screen, FPL 62064 exhibits the same inhibitory activity against prostaglandin synthase (IC50 for seminal vesicle prostaglandin synthetase is 3.1 μM) and 5-1 cyclooxygenase (IC50 for RBL-1 cytosolic 5-1 cyclooxygenase is 3.5 μM). On the other hand, FPL 62064 more easily inhibited prostaglandin synthase (IC50 of 3.6 μM) in undamaged RBL-I cells than it did 5-1 cyclooxygenase (IC50 of 31 μM). In mouse macrophages, leukotrienes (IC50 0.72 μM) and prostaglandins (IC50 0.43 μM) yield IC50s that are identical, indicating that there is no discernible difference in sensitivity [1].
ln Vivo
Immunoglobulin-induced peritoneal inflammation in female LACA mice is inhibited by treatment with FPL 62064 (5–20 mg/kg; i.p.) [1].
Animal Protocol
Animal/Disease Models: Female LACA mice (20-30 g) injected with immune complexes [1].
Doses: 5 mg/kg, 10 mg/kg, 20 mg/kg
Route of Administration: intraperitoneal (ip) injection
Experimental Results: Dose-related inhibition of dye extravasation, leukotriene C4 (LTC4) and prostaglandin E2 (PGE2) formation effect.
References

[1]. FPL 62064, a topically active 5-lipoxygenase/cyclooxygenase inhibitor. Agents Actions. 1990 Jun;30(3-4):432-42.

[2]. Synthesis and biological evaluation of pyrazolone analogues as potential anti-inflammatory agents targeting cyclooxygenases and 5-lipoxygenase. Arch Pharm (Weinheim). 2020 Feb 7:e1900308.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C₁₆H₁₅N₃O
Molecular Weight
265.31
Exact Mass
265.121
CAS #
103141-09-9
PubChem CID
128268
Appearance
Light yellow to brown solid powder
Density
1.2±0.1 g/cm3
Boiling Point
442.6±25.0 °C at 760 mmHg
Flash Point
221.5±23.2 °C
Vapour Pressure
0.0±1.1 mmHg at 25°C
Index of Refraction
1.610
LogP
3.49
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
3
Rotatable Bond Count
4
Heavy Atom Count
20
Complexity
285
Defined Atom Stereocenter Count
0
Synonyms
FPL 62064; FPL-62064
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~250 mg/mL (~942.29 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 1.67 mg/mL (6.29 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 1.67 mg/mL (6.29 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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