1196070-26-4

1196070-26-4 structure

Name: GSK2190915 (sodium salt)
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
CAS Number: 1196070-26-4
Molecular Formula: C₃₈H₄₂N₃NaO₄S
Molecular Weight: 659.81300
Catalog: Signaling Pathways Immunology/Inflammation FLAP
Create Date: 2017-05-13 05:04:12
Modify Date: 2024-01-06 17:41:10
Fiboflapon sodium (GSK2190915 (sodium salt)) is a potent FLAP(5-Lipoxygenase-activating protein) inhibitor with binding IC50 of 2.9 nM.

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
Synonyms	FIBOFLAPON SODIUM AM803 sodium salt AM803 sodium UNII-75YS00XOG3 GSK2190915 (sodium salt)

Description	Fiboflapon sodium (GSK2190915 (sodium salt)) is a potent FLAP(5-Lipoxygenase-activating protein) inhibitor with binding IC50 of 2.9 nM.
Related Catalog	Signaling Pathways >> Immunology/Inflammation >> FLAP Research Areas >> Inflammation/Immunology
Target	IC50: 76 nM (inhibition of LTB4 in human blood 5 h incubation)[1].
In Vitro	Fiboflapon (AM803) exhibits excellent preclinical toxicology and pharmacokinetics in rat and dog. Fiboflapon (AM803) also demonstrated an extended pharmacodynamic effect in a rodent bronchoalveolar lavage (BAL) model[1]. Oral administration of Fiboflapon (AM803) (1 mg/kg) resulted in sustained inhibition of ex vivo ionophore-challenged whole blood LTB4 biosynthesis with >90% inhibition for up to 12 h and an EC50 of approximately 7 nM. When rat lungs were challenged in vivo with calcium-ionophore, Fiboflapon (AM803) inhibited LTB4 and cysteinyl leukotriene (CysLT) production with ED50s of 0.12 mg/kg and 0.37 mg/kg, respectively. The inhibition measured 16 h following a single oral dose of 3 mg/kg was 86% and 41% for LTB4 and CysLTs, respectively. In an acute inflammation setting, Fiboflapon (AM803) dose-dependently reduced LTB4, CysLTs, plasma protein extravasation and neutrophil influx induced by peritoneal zymosan injection. Finally, AM803 increased survival time in mice exposed to a lethal intravenous injection of platelet activating factor (PAF)[2].
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	C₃₈H₄₂N₃NaO₄S
Molecular Weight	659.81300
Exact Mass	659.27900
PSA	114.60000
LogP	7.64190

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