| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Fiboflapon sodium (also known as AM-803 and GSK2190915 sodium) is a novel,orally bioavailable and potent FLAP (5-Lipoxygenase-activating protein) inhibitor with binding IC50 of 2.9 nM. Fiboflapon attenuated the early (0-2 h) and late (4-10 h) asthmatic responses to inhaled allergen compared with placebo. GSK2190915 shows potential as a treatment for patients with asthma. Efficacy was demonstrated for GSK2190915 30 mg compared with placebo in day-time symptom scores and day-time SABA use.
| 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].
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| References |
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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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