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Fiboflapon sodium

Catalog No. T11487L CAS 1196070-26-4

Synonyms: 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.

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Fiboflapon sodium, CAS 1196070-26-4

Pack Size	Availability	Price/USD
2 mg	5 days	$ 89.00
25 mg	8-10 weeks	$ 635.00
50 mg	8-10 weeks	$ 825.00
100 mg	8-10 weeks	$ 1,240.00

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Biological Description

Chemical Properties

Storage & Solubility Information

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
Molecular Weight	660.83
Formula	C38H43N3NaO4S
CAS No.	1196070-26-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 32 mg/mL (48.50 mM)

References and Literature

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.

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Keywords

Fiboflapon sodium 1196070-26-4 Immunology/Inflammation LTR GSK2190915 sodium salt GSK2190915 sodium AM-803 sodium inhibitor inhibit

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