Identification | Back Directory | [Name]
GSK2190915 (sodiuM salt) | [CAS]
1196070-26-4 | [Synonyms]
GSK-2190915A AM-803 sodium) Fiboflapon sodium GSK2190915 Sodium GSK2190915 (sodiuM salt) GSK2190915 sodium
(GSK-2190915A FIBOFLAPON SODIUM;FIBOFLAPON SODIUM | [Molecular Formula]
C38H44N3NaO4S | [MOL File]
1196070-26-4.mol | [Molecular Weight]
661.84 |
Hazard Information | Back Directory | [Uses]
Fiboflapon sodium (GSK2190915; AM-803) is a potent and 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[1]. | [IC 50]
LTB4: 76 nM (IC50) | [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. DOI:10.1021/jm2008369 [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. DOI:10.1016/j.ejphar.2010.05.003 |
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