| Identification | Back Directory | [Name]
GSK2190915 | [CAS]
936350-00-4 | [Synonyms]
AM 803
GSK2190915
fiboflapon
GSK2190915 (AM803)
AM-803;FIBOFLAPON;GSK-2190915
1H-Indole-2-propanoic acid, 3-[(1,1-dimethylethyl)thio]-1-[[4-(6-ethoxy-3-pyridinyl)phenyl]methyl]-α,α-dimethyl-5-[(5-methyl-2-pyridinyl)methoxy]-
3-[(1,1-Dimethylethyl)thio]-1-[[4-(6-ethoxy-3-pyridinyl)phenyl]methyl]-alpha,alpha-dimethyl-5-[(5-methyl-2-pyridinyl)methoxy]-1H-indole-2-propanoic acid | [Molecular Formula]
C38H43N3O4S | [MOL File]
936350-00-4.mol | [Molecular Weight]
637.83 |
| Chemical Properties | Back Directory | [Boiling point ]
796.3±60.0 °C(Predicted) | [density ]
1.16±0.1 g/cm3(Predicted) | [solubility ]
DMSO: soluble; Methanol: soluble | [form ]
A crystalline solid | [pka]
4.70±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Fiboflapon (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]. | [Definition]
ChEBI:Fiboflapon is a phenylpyridine. | [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]. | [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 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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Musechem
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InvivoChem
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