| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
FPL 62064 targets 5-lipoxygenase (5-LOX) and cyclooxygenase (COX, prostaglandin synthetase). It inhibits RBL-1 cytosolic 5-lipoxygenase with an IC50 of 3.5 μM and seminal vesicle prostaglandin synthetase with an IC50 of 3.1 μM. This dual inhibition makes it a valuable tool for studying the inflammatory process.
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| 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].
In vitro, FPL 62064 potently inhibits 5-lipoxygenase with an IC50 of 3.5 μM and COX with an IC50 of 3.1 μM. It is a potent dual inhibitor of these two key enzymes involved in inflammatory processes. Its activity makes it a valuable tool for studying the arachidonic acid cascade and inflammation. |
| ln Vivo |
Immunoglobulin-induced peritoneal inflammation in female LACA mice is inhibited by treatment with FPL 62064 (5–20 mg/kg; i.p.) [1].
In vivo, FPL 62064 has potent anti-inflammatory activity. As a dual 5-LOX/COX inhibitor, it can be administered to animal models of inflammation to study its effects on inflammatory responses. Its ability to inhibit both enzymes in the arachidonic acid cascade translates to in vivo anti-inflammatory efficacy. |
| Enzyme Assay |
In vitro enzyme assays for FPL 62064 involve measuring its inhibition of 5-lipoxygenase and COX activities. 5-LOX activity is measured using RBL-1 cytosolic preparations with arachidonic acid as substrate, and product formation is measured by HPLC or spectrophotometry. COX activity is measured using seminal vesicle preparations, and prostaglandin production is measured by ELISA or radioimmunoassay.
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| Cell Assay |
For in vitro cell-based assays, immune cells (e.g., macrophages, leukocytes) are cultured and treated with FPL 62064 at various concentrations. The compound's effects on leukotriene and prostaglandin production are measured by ELISA. Cell viability is assessed by standard assays. Its anti-inflammatory effects are assessed by measuring cytokine production.
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| 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. In vivo animal studies with FPL 62064 are conducted in models of inflammation. The compound is administered orally or intraperitoneally to rodents. Efficacy is measured by assessing inflammatory markers, tissue damage, or disease severity. Its anti-inflammatory effects have been demonstrated in various preclinical models. |
| ADME/Pharmacokinetics |
FPL 62064 (CAS: 103141-09-9) has a molecular weight of 307.35 g/mol and a molecular formula of C16H17N3O2. Chemical name: N-(4-methoxyphenyl)-1-phenyl-1H-pyrazol-3-amine. Appearance: solid powder. Purity: ≥98%. Solubility: DMSO. Storage: -20°C.
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| Toxicity/Toxicokinetics |
FPL 62064 is a research compound and is not approved for human therapeutic use. In preclinical studies, it has shown a manageable safety profile. As a dual 5-LOX/COX inhibitor, it may have effects on normal inflammatory responses. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
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| Additional Infomation |
FPL 62064 is a potent dual inhibitor of 5-lipoxygenase (5-LOX) and cyclooxygenase (COX) with IC50 values of 3.5 μM and 3.1 μM, respectively. It exhibits potent anti-inflammatory activity. It is not FDA-approved and is intended for research use only.
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| Molecular Formula |
C₁₆H₁₅N₃O
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|---|---|
| Molecular Weight |
265.31
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| Exact Mass |
265.121
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| CAS # |
103141-09-9
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| PubChem CID |
128268
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| Appearance |
Light yellow to brown solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
442.6±25.0 °C at 760 mmHg
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| Flash Point |
221.5±23.2 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.610
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| LogP |
3.49
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
20
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| Complexity |
285
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| Defined Atom Stereocenter Count |
0
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| Synonyms |
FPL 62064; FPL-62064
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~942.29 mM)
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| 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.
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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