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Fiboflapon

Fiboflapon
Fiboflapon (GSK2190915) is an orally available and effective 5-lipoxygenase-activating protein (FLAP) inhibitor that binds FLAP with a titer of 2.9 nM and inhibition of LTB4 in human blood with an IC50 of 76 nM.
Catalog No. T11487Cas No. 936350-00-4
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Purity:97.01%
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Fiboflapon

Purity: 97.01%
Catalog No. T11487Alias GSK2190915, AM-803Cas No. 936350-00-4

Fiboflapon (GSK2190915) is an orally available and effective 5-lipoxygenase-activating protein (FLAP) inhibitor that binds FLAP with a titer of 2.9 nM and inhibition of LTB4 in human blood with an IC50 of 76 nM.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
1 mg$51In Stock
5 mg$123In Stock
10 mg$198In Stock
25 mg$393In Stock
50 mg$645In Stock
1 mL x 10 mM (in DMSO)$173In Stock
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Product Introduction

Bioactivity
Description
Fiboflapon (GSK2190915) is an orally available and effective 5-lipoxygenase-activating protein (FLAP) inhibitor that binds FLAP with a titer of 2.9 nM and inhibition of LTB4 in human blood with an IC50 of 76 nM.
Targets&IC50
LTB4:76 nM
In vitro
Fiboflapon (AM-803) demonstrates excellent preclinical toxicology and pharmacokinetics in both rats and dogs. In the rodent bronchoalveolar lavage (BAL) model, Fiboflapon (AM-803) also exhibits prolonged pharmacological effects[2].
In vivo
Orally administered at 1 mg/kg, Fiboflapon (AM-803) sustains a continuous inhibition of ex vivo ionophore-stimulated whole blood leukotriene B4 (LTB4) biosynthesis, with an inhibition rate exceeding 90% for up to 12 hours, and an EC50 of approximately 7 nM. When rat lungs are subjected to in vivo calcium ionophore challenge, Fiboflapon (AM-803) inhibits the production of LTB4 and cysteinyl leukotrienes (CysLT) with ED50 values of 0.12 mg/kg and 0.37 mg/kg, respectively. Following a single oral dose of 3 mg/kg, the inhibition rates measured 16 hours later for LTB4 and CysLT are 86% and 41%, respectively. In an acute inflammatory environment, Fiboflapon dose-dependently reduces LTB4, CysLT, plasma protein extravasation, and neutrophil influx induced by intraperitoneal yeast glucan injection. Lastly, Fiboflapon increases the survival time of mice exposed to intravenous injection of lethal platelet-activating factor (PAF) [2].
AliasGSK2190915, AM-803
Chemical Properties
Molecular Weight637.83
FormulaC38H43N3O4S
Cas No.936350-00-4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 40 mg/mL (62.71 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.5678 mL7.8391 mL15.6782 mL78.3908 mL
5 mM0.3136 mL1.5678 mL3.1356 mL15.6782 mL
10 mM0.1568 mL0.7839 mL1.5678 mL7.8391 mL
20 mM0.0784 mL0.3920 mL0.7839 mL3.9195 mL
50 mM0.0314 mL0.1568 mL0.3136 mL1.5678 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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