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Purity: ≥98%
Fiboflapon (also known as AM-803 and GSK2190915) 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 |
Fiboflapon (AM-803) showed good pharmacokinetics and preclinical toxicity in dogs and storage. Moreover, fibroflapon (AM-803) shows protracted pharmacokinetics in the bronchoalveolar lavage (BAL) model of cryodont death. Efficacious outcomes [1].
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| ln Vivo |
Fiboflapon (AM-803: 1 mg/kg) has an EC50 of roughly 7 nM and persistently suppresses the production of LTB4 in whole blood when stimulated with an ionophore by >90% for up to 12 hours. Fiboflapon (AM-803) stops the formation of cysteine polystyrene leukotriene (CysLT) and LTB4 in the downstream lungs when they are internally challenged with calcium ionophores, with an ED50 of 0.12 mg/kg and 0.37 mg/kg, respectively. The LTB4 and CysLT mice models showed 86% and 41% inhibition rates, respectively, 16 hours after a single 3 mg/kg dosage. LTB4, CysLT, PBS extravasation, and neutrophil influx caused by peritoneal yeast reverse injection were all dose-dependently decreased by fibroflapon in acute environmental conditioning. And last, Fiboflapon lengthens the time needed for intravenous fatal activating factor (PAF) to sterilize [1].
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| References |
[1]. Stock NS, et al. 5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhibitor. J Med Chem. 2011 Dec 8;54(23):8013-29.
[2]. Lorrain DS, et al. Pharmacology of AM803, a novel selective five-lipoxygenase-activating protein (FLAP) inhibitor in rodent models of acute inflammation. Eur J Pharmacol. 2010 Aug 25;640(1-3):211-8. |
| Molecular Formula |
C38H43N3O4S
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|---|---|
| Molecular Weight |
637.8307
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| CAS # |
936350-00-4
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| Related CAS # |
Fiboflapon sodium;1196070-26-4
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| SMILES |
S(C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])C1C2C([H])=C(C([H])=C([H])C=2N(C([H])([H])C2C([H])=C([H])C(C3=C([H])N=C(C([H])=C3[H])OC([H])([H])C([H])([H])[H])=C([H])C=2[H])C=1C([H])([H])C(C(=O)O[H])(C([H])([H])[H])C([H])([H])[H])OC([H])([H])C1C([H])=C([H])C(C([H])([H])[H])=C([H])N=1
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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 : ~50 mg/mL (~78.39 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.92 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: 10 mg/mL (15.68 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5678 mL | 7.8391 mL | 15.6782 mL | |
| 5 mM | 0.3136 mL | 1.5678 mL | 3.1356 mL | |
| 10 mM | 0.1568 mL | 0.7839 mL | 1.5678 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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