糠酸氟替卡松

中文名称:

糠酸氟替卡松

中文同义词:

糠酸氟替卡松;氟替卡松糠酸酯;糠酸氟替卡松-[D3]

英文名称:

FLUTICASONE FUROATE

英文同义词:

FLUTICASONE FUROATE;Androsta-1,4-diene-17-carbothioic acid, 6,9-difluoro-17-((2- furanylcarbonyl)oxy)-11-hydroxy-16-methyl-3-oxo-, S-(fluoromethyl) ester, (6alpha,11beta,16alpha,17alpha)-;Gw 685698x;Unii-js86977wnv;Veramyst;(6α,11β,16α,17α)-6,9-Difluoro-17-[(2-furanylcarbonyl)oxy]-11-hydroxy-16-Methyl-3-oxoandrosta-1,4-diene-17-carbothioic Acid S-(FluoroMethyl) Ester;AllerMist;AvaMys

CAS号:

397864-44-7

分子式:

C27H29F3O6S

分子量:

538.58

EINECS号:

222-789-2

相关类别:

医药原料;原料药;医用原料;化工原料;Intermediates Fine Chemicals;Pharmaceuticals;Steroids

Mol文件:

397864-44-7.mol

沸点 

625.2±55.0 °C(Predicted)

密度 

1.39

酸度系数(pKa)

12.52±0.70(Predicted)

生物活性

Fluticasone furoate (GW685698)是一种吸入性皮质类固醇/长效的β肾上腺素能受体激动剂的复方治疗药物，能延长支气管扩张剂的作用时间。它被用于非过敏性和过敏性皮炎的治疗。

靶点

Kd: 0.3 nM (Corticosteroid)

体外研究

Fluticasone furoate comes in a nasal spray, as an aqueous suspension of micronized fluticasone furoate for topical administration to the nasal mucosa by means of a metering, atomizing spray pump. Fluticasone furonate displays great potency in inhibiting tumor necrosis factor synthesis and action. Fluticasone furonate is also potent in preventing damage to cultured human lung epithelial cells by different stimulus.

体内研究

Fluticasone furonate is 99.4% bound to plasma protein in vitro and other research indicated extensive first-pass metabolism of the absorbed drug. Protein binding is highly relevant because only the unbound free drug can exert an effect at the receptor site. Clearance of Fluticasone furonate is primarily by hydrolysis in the liver by the cytochrome P450 isozyme (CYP) 3A4 that converts the drug to the 17β-carboxylic acid metabolite (M10), which displays low glucocorticoid receptor agonist potency. Fluticasone furonate is excreted mainly in the feces, with only minor amounts in the urine.