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| | GSK2190915 Basic information |
| Product Name: | GSK2190915 | | Synonyms: | GSK2190915;GSK2190915 (AM803);AM 803;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;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]-;Fiboflapon, 10 mM in DMSO;Fiboflapon (GSK2190915) | | CAS: | 936350-00-4 | | MF: | C38H43N3O4S | | MW: | 637.83 | | EINECS: | | | Product Categories: | | | Mol File: | 936350-00-4.mol |  |
| | GSK2190915 Chemical Properties |
| 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 |
| | GSK2190915 Usage And Synthesis |
| 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 |
| | GSK2190915 Preparation Products And Raw materials |
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