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Fiboflapon sodium
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Fiboflapon sodium图片
CAS NO:1196070-26-4
包装:50 mg
市场价:7419元

产品名称
GSK2190915 sodium salt
AM-803 sodium
产品介绍

产品描述

Fiboflapon sodium (GSK2190915) is an 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.

体外活性

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).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.?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.

Cas No.

1196070-26-4

分子式

C38H43N3NaO4S

分子量

660.82

别名

GSK2190915 sodium salt;AM-803 sodium

储存和溶解度

DMSO:32 mg/mL (48.50 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years