GSK2190915 (sodium salt)

Modify Date: 2024-01-06 17:41:10

GSK2190915 (sodium salt) Structure
GSK2190915 (sodium salt) structure
Common Name GSK2190915 (sodium salt)
CAS Number 1196070-26-4 Molecular Weight 659.81300
Density N/A Boiling Point N/A
Molecular Formula C38H42N3NaO4S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of GSK2190915 (sodium salt)


Fiboflapon sodium (GSK2190915 (sodium salt)) is a potent FLAP(5-Lipoxygenase-activating protein) inhibitor with binding IC50 of 2.9 nM.

 Names

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
Synonym More Synonyms

 GSK2190915 (sodium salt) Biological Activity

Description Fiboflapon sodium (GSK2190915 (sodium salt)) is a potent FLAP(5-Lipoxygenase-activating protein) inhibitor with binding IC50 of 2.9 nM.
Related Catalog
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.

 Chemical & Physical Properties

Molecular Formula C38H42N3NaO4S
Molecular Weight 659.81300
Exact Mass 659.27900
PSA 114.60000
LogP 7.64190

 Synonyms

FIBOFLAPON SODIUM
AM803 sodium salt
AM803 sodium
UNII-75YS00XOG3
GSK2190915 (sodium salt)
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Price: $219/10mM*1mLinDMSO

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