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Fiboflapon sodium

CAS No. : 1196070-26-4

MCE 站：Fiboflapon sodium

产品活性：Fiboflapon sodium (GSK2190915; AM-803) 是一种口服有效的 5-脂氧合酶激活蛋白 (FLAP) 抑制剂，结合 FLAP 的效价为 2.9 nM，在人血中抑制 LTB4 的 IC₅₀ 为 76 nM。

研究领域：Immunology/Inflammation  |  GPCR/G Protein

作用靶点：FLAP  |  Leukotriene Receptor

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. 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).

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