GSK2190915 (sodium salt)
Modify Date: 2024-01-06 17:41:10
GSK2190915 (sodium salt) structure
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Common Name | GSK2190915 (sodium salt) | ||
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| 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. |
| 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 |
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| Synonym | More Synonyms |
| Description | Fiboflapon sodium (GSK2190915 (sodium salt)) is a potent FLAP(5-Lipoxygenase-activating protein) inhibitor with binding IC50 of 2.9 nM. |
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| 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 |
| Molecular Formula | C38H42N3NaO4S |
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| Molecular Weight | 659.81300 |
| Exact Mass | 659.27900 |
| PSA | 114.60000 |
| LogP | 7.64190 |
| FIBOFLAPON SODIUM |
| AM803 sodium salt |
| AM803 sodium |
| UNII-75YS00XOG3 |
| GSK2190915 (sodium salt) |