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Fiboflapon sodium

Name: Fiboflapon sodium
Brand: TargetMol
SKU: T11487L
Rating: 4.5 (1 reviews)

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Catalog No. T11487LCas No. 1196070-26-4

Alias GSK2190915 sodium salt, AM-803 sodium

Fiboflapon sodium (GSK2190915) is an orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.

Fiboflapon sodium

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Catalog No. T11487LAlias GSK2190915 sodium salt, AM-803 sodiumCas No. 1196070-26-4

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$89	5 days	5 days
25 mg	$635	8-10 weeks	8-10 weeks
50 mg	$825	8-10 weeks	8-10 weeks
100 mg	$1,240	8-10 weeks	8-10 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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.

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Product Introduction

Bioactivity

Description	Fiboflapon sodium (GSK2190915) is an orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
Targets&IC50	LTB4:76 nM
In vitro	In vivo studies revealed that Fiboflapon (AM803) effectively inhibits the production of LTB4 and cysteinyl leukotriene (CysLT) in rat lungs challenged with calcium-ionophore, showing ED50 values of 0.12 mg/kg and 0.37 mg/kg, respectively. Following a single oral dose of 3 mg/kg, inhibition levels 16 hours post-administration were 86% for LTB4 and 41% for CysLTs. In scenarios of acute inflammation, Fiboflapon (AM803) demonstrated a dose-dependent reduction in LTB4, CysLTs, plasma protein extravasation, and neutrophil influx following peritoneal zymosan injection. Furthermore, AM803 significantly prolonged survival in mice after a lethal dose of platelet-activating factor (PAF) intravenously. Fiboflapon (AM803) has shown excellent preclinical toxicology and pharmacokinetics in rats and dogs, alongside a remarkable pharmacodynamic extension in a rodent bronchoalveolar lavage (BAL) model. Oral administration at 1 mg/kg led to a sustained inhibition of LTB4 biosynthesis in ex vivo ionophore-challenged whole blood, with over 90% inhibition lasting up to 12 hours and an EC50 of approximately 7 nM.
Synonyms	GSK2190915 sodium salt, AM-803 sodium

Chemical Properties

Molecular Weight	660.83
Formula	C₃₈H₄₃N₃NaO₄S
Cas No.	1196070-26-4
Smiles	[Na].CCOc1ccc(cn1)-c1ccc(Cn2c(CC(C)(C)C(O)=O)c(SC(C)(C)C)c3cc(OCc4ccc(C)cn4)ccc23)cc1jcExt:v:0:0
Relative Density.	1.31g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 32 mg/mL (48.42 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.5132 mL	7.5662 mL	15.1325 mL	75.6624 mL
5 mM	0.3026 mL	1.5132 mL	3.0265 mL	15.1325 mL
10 mM	0.1513 mL	0.7566 mL	1.5132 mL	7.5662 mL
20 mM	0.0757 mL	0.3783 mL	0.7566 mL	3.7831 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc