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Fiboflapon, 5-脂氧合酶活化蛋白抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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 IC 50 of 76 nM for inhibition of LTB4 in human blood
In Vitro
Fiboflapon (AM-803) exhibits excellent preclinical toxicology and pharmacokinetics in rat and dog. Fiboflapon (AM-803) also demonstrated an extended pharmacodynamic effect in a rodent bronchoalveolar lavage (BAL) model . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 EC 50 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 ED 50 s 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) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:LTB 4 76 nM (IC 50 )
规格
别名
纤维瓣
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Fiboflapon
生化机理
Fiboflapon（GSK2190915；AM-803）是一种口服生物活性强的 5-脂氧合酶激活蛋白（FLAP）抑制剂，与 FLAP 结合的效力为 2.9 nM，抑制人体血液中 LTB4 的 IC 50 为 76 nM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
5-脂氧合酶活化蛋白抑制剂
名称和识别符
EC号
689-174-2
分子类型
小分子
Isomeric SMILES
CCOC1=NC=C(C=C1)C2=CC=C(C=C2)CN3C4=C(C=C(C=C4)OCC5=NC=C(C=C5)C)C(=C3CC(C)(C)C(=O)O)SC(C)(C)C
PubChem CID
分子量
637.83
技术文档
高级数据
质检证书（CoA,COO,BSE/TSE 和分析图谱)
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溶液计算器
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