936350-00-4

936350-00-4 structure

Name: GSK2190915
Chemical Name: 3-[3-tert-butylsulfanyl-1-[[4-(6-ethoxypyridin-3-yl)phenyl]methyl]-5-[(5-methylpyridin-2-yl)methoxy]indol-2-yl]-2,2-dimethylpropanoic acid
CAS Number: 936350-00-4
Molecular Formula: C₃₈H₄₃N₃O₄S
Molecular Weight: 637.83100
Catalog: Signaling Pathways Immunology/Inflammation FLAP
Create Date: 2017-09-16 16:41:27
Modify Date: 2024-01-16 20:08:50
Fiboflapon (GSK2190915) is a potent FLAP(5-Lipoxygenase-activating protein) inhibitor with binding IC50 of 2.9 nM.

Name	3-[3-tert-butylsulfanyl-1-[[4-(6-ethoxypyridin-3-yl)phenyl]methyl]-5-[(5-methylpyridin-2-yl)methoxy]indol-2-yl]-2,2-dimethylpropanoic acid
Synonyms	FIBOFLAPON AM 803 Fiboflapon (USAN) UNII-Y1NA96IX3T Fiboflapon [USAN:INN] GSK2190915

Description	Fiboflapon (GSK2190915) 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 (AM-803) exhibits excellent preclinical toxicology and pharmacokinetics in rat and dog. Fiboflapon (AM-803) also demonstrated an extended pharmacodynamic effect in a rodent bronchoalveolar lavage (BAL) model [1].
In Vivo	Oral administration of Fiboflapon (AM-803: 1 mg/kg) results 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 are challenged in vivo with calcium-ionophore, Fiboflapon (AM-803) inhibits 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 dose-dependently reduced LTB4, CysLTs, plasma protein extravasation and neutrophil influx induced by peritoneal zymosan injection. Finally, Fiboflapon increases survival time in mice exposed to a lethal intravenous injection of platelet activating factor (PAF)[1].
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
Molecular Weight	637.83100
Exact Mass	637.29700
PSA	111.77000
LogP	8.97660

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