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Product details

名称

Fiboflapon, 5-脂氧合酶活化蛋白抑制剂

分子类型

小分子

别名

纤维瓣

英文别名

英文名称

Fiboflapon

货号

F649894-5mg

包装规格

5mg

浓度

≥98%

储存温度

-20°C储存

运输条件

超低温冰袋运输

产品介绍

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. Form:Solid IC50& Target:LTB 4 76 nM (IC 50 )

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。

CAS号

936350-00-4

分子式

C38H43N3O4S

分子量

637.83 g/mol

PubChem编号

44473151

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

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

44473151

溶解性

DMSO : 50 mg/mL (78.39 mM; Need ultrasonic)

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

637.297 Da

单同位素质量Monoisotopic Mass

637.297 Da

拓扑极表面积Topological Polar Surface Area

112.000 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

966

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

7.8

作用类型

抑制剂

作用机制

5-脂氧合酶活化蛋白抑制剂

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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