| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Fiboflapon Sodium targets 5-lipoxygenase-activating protein (FLAP), an integral membrane protein that is required for the activity of 5-lipoxygenase (5-LOX). FLAP is responsible for the transfer of arachidonic acid to 5-LOX, the enzyme that catalyzes the first two steps in the biosynthesis of leukotrienes, which are potent pro-inflammatory lipid mediators. By inhibiting FLAP, Fiboflapon Sodium prevents the production of leukotrienes, reducing inflammation.
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| ln Vitro |
In rats and dogs, fibroflapon (AM803) has shown outstanding preclinical toxicity and pharmacokinetics. The rodent bronchoalveolar lavage (BAL) paradigm shows sustained pharmacodynamic effects when fibroflapon (AM803) is administered [1]. In ex vivo whole blood that has been challenged with an ionophore, oral administration of Fiboflapon (AM803) (1 mg/kg) sustainably reduces LTB4 production by >90% for 12 hours, with an EC50 of roughly 7 nM. Fiboflapon (AM803) suppressed the synthesis of cysteinyl leukotriene (CysLT) and LTB4 in rat lungs when they were exposed to calcium ionophores in vivo, with an ED50 of 0.12 mg/kg and 0.37 mg/kg, respectively. 16 hours following a single oral dose of 3 mg/kg, the inhibition of LTB4 and CysLT was 86% and 41%, respectively. In an acute inflammatory context, intraperitoneal zymosan injection-induced LTB4, CysLT, plasma protein extravasation, and neutrophil influx are all reduced in a dose-dependent manner by fibroflapon (AM803). Ultimately, mice given deadly intravenous infusions of platelet-activating factor (PAF) were able to survive longer when given AM803 [2].
In vitro, Fiboflapon Sodium is a potent FLAP inhibitor with a binding IC50 of 2.9 nM. As a FLAP inhibitor, the compound effectively blocks leukotriene biosynthesis. The compound's potency and selectivity for FLAP make it a valuable tool for studying the role of leukotrienes in inflammatory diseases such as asthma. |
| ln Vivo |
In vivo, Fiboflapon Sodium is an orally bioavailable FLAP inhibitor with potential for the treatment of asthma. By inhibiting FLAP and reducing leukotriene production, the compound is expected to have anti-inflammatory activity in respiratory diseases. Specific animal model data are not detailed in the available sources.
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| Enzyme Assay |
The FLAP binding assay for Fiboflapon Sodium involves incubating the compound with membrane preparations from cells expressing human FLAP and a radiolabeled FLAP ligand. After incubation, bound and free ligands are separated by filtration, and the radioactivity is counted. The IC50 for displacement of the radioligand is calculated from the competition curve.
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| Cell Assay |
To evaluate the cellular activity of Fiboflapon Sodium, cells that produce leukotrienes (such as human polymorphonuclear leukocytes or mast cells) are treated with varying concentrations of the compound and stimulated with a calcium ionophore (such as A23187) to induce leukotriene production. The levels of leukotrienes (such as LTB4 or LTC4) in the cell supernatant are measured using ELISA or LC-MS/MS. The IC50 for inhibition of leukotriene production is calculated.
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| Animal Protocol |
Specific in vivo animal experiment protocols for Fiboflapon Sodium are not detailed in the available sources. As a FLAP inhibitor, the compound would typically be evaluated in animal models of inflammation, such as ovalbumin-induced airway inflammation or LPS-induced lung inflammation. Animals would be treated with Fiboflapon Sodium orally, and inflammatory parameters (such as leukocyte infiltration and leukotriene levels) would be measured.
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| ADME/Pharmacokinetics |
Fiboflapon Sodium is characterized as being orally bioavailable. Specific pharmacokinetic parameters (e.g., Cmax, Tmax, half-life, AUC) are not detailed in the available sources. The compound has a molecular weight of 659.82 and a molecular formula of C38H42N3NaO4S. It is soluble in DMSO. As a powder, it is stable at -20°C for 3 years.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Fiboflapon Sodium are not provided in the available sources. As a research compound, it is intended for laboratory use only and is not approved for human therapeutic applications. The compound is a potent FLAP inhibitor, and its toxicity profile would be expected to be consistent with other FLAP inhibitors. Standard safety precautions should be followed when handling this compound.
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| References |
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| Additional Infomation |
Fiboflapon Sodium is also known as AM-803 and GSK2190915 sodium. It is a novel, orally bioavailable, and potent FLAP (5-Lipoxygenase-activating protein) inhibitor with a binding IC50 of 2.9 nM. It is a 5-lipoxygenase inhibitor potentially for the treatment of asthma. The compound has a molecular formula of C38H42N3NaO4S and a molecular weight of 659.82.
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| Molecular Formula |
C38H42N3O4S-.NA+
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|---|---|
| Molecular Weight |
659.813
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| Exact Mass |
659.279
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| CAS # |
1196070-26-4
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| Related CAS # |
Fiboflapon;936350-00-4
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| PubChem CID |
44473150
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| Appearance |
White to off-white solid powder
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| LogP |
7.641
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
47
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| Complexity |
973
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NOJNFULGOQGBKB-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C38H43N3O4S.Na/c1-8-44-34-18-14-28(22-40-34)27-12-10-26(11-13-27)23-41-32-17-16-30(45-24-29-15-9-25(2)21-39-29)19-31(32)35(46-37(3,4)5)33(41)20-38(6,7)36(42)43;/h9-19,21-22H,8,20,23-24H2,1-7H3,(H,42,43);/q;+1/p-1
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| Chemical Name |
sodium;3-[3-tert-butylsulfanyl-1-[[4-(6-ethoxypyridin-3-yl)phenyl]methyl]-5-[(5-methylpyridin-2-yl)methoxy]indol-2-yl]-2,2-dimethylpropanoate
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~100 mg/mL (~151.56 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (3.79 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (3.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5156 mL | 7.5779 mL | 15.1559 mL | |
| 5 mM | 0.3031 mL | 1.5156 mL | 3.0312 mL | |
| 10 mM | 0.1516 mL | 0.7578 mL | 1.5156 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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