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名称

Fiboflapon sodium, 5-脂氧合酶活化蛋白抑制剂

分子类型

小分子

别名

菲博拉平钠

英文别名

英文名称

Fiboflapon sodium

货号

F647997-5mg

包装规格

5mg

浓度

≥99%

储存温度

2-8°C储存,干燥

运输条件

冰袋运输

产品介绍

Fiboflapon sodium (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 (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 EC 50 of approximately 7 nM. When rat lungs were challenged in vivo with calcium-ionophore, Fiboflapon (AM803) inhibited 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 (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). 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 sodium（GSK2190915；AM-803）是一种强效的口服生物活性 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

1196070-26-4

分子式

C38H42N3NaO4S

分子量

659.81 g/mol

EC号

689-173-7

PubChem编号

44473150

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.[Na+]

IIUPAC Name

sodium;3-[3-tert-butylsulfanyl-1-[[4-(6-ethoxypyridin-3-yl)phenyl]methyl]-5-[(5-methylpyridin-2-yl)methoxy]indol-2-yl]-2,2-dimethylpropanoate

INCHI

1S/C38H43N3O4S.Na/c1-8-44-34-18-14-28(22-40-34)27-12-10-26(11-13-27)23-41-32-17-16-30(45-24-29-15-9-25(2)21-39-29)19-31(32)35(46-37(3,4)5)33(41)20-38(6,7)36(42)43;/h9-19,21-22H,8,20,23-24H2,1-7H3,(H,42,43);/q;+1/p-1

InChi Key

NOJNFULGOQGBKB-UHFFFAOYSA-M

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.[Na+]

PubChem CID

44473150

关联CAS

1196070-26-4

溶解性

DMSO : 100 mg/mL (151.56 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

659.279 Da

单同位素质量Monoisotopic Mass

659.279 Da

拓扑极表面积Topological Polar Surface Area

115.000 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

973.000

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

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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