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CAS No. : 1196070-26-4
MCE 国际站: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).
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Anti-COVID-19 Compound Library | Orally Active Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | Masilukast | MK-886 | FEN1-IN-4 | CP-96021 hydrochloride | CAY10583 | Olsalazine | U-75302 | Pranlukast | Amelubant | (S)-Verapamil-d7 hydrochloride | Zafirlukast-d7 | Quininib | AM103 | RS-601 | Tipelukast | LM-1484 | RG-12525 | Quinotolast sodium | Darbufelone mesylate | Montelukast sodium | Ablukast | Chamazulene | Fiboflapon | CP-105696 | LTB4 antagonist 2 | ONO4057 | Pranlukast-d4 | FEN1-IN-1 | AM679
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
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货号: HY-15874A
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