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397864-44-7

中文名称 糠酸氟替卡松
英文名称 FLUTICASONE FUROATE
CAS 397864-44-7
分子式 C27H29F3O6S
分子量 538.58
MOL 文件 397864-44-7.mol
更新日期 2024/05/28 11:40:31
397864-44-7 结构式 397864-44-7 结构式

基本信息

中文别名
糠酸氟替卡松
氟替卡松糠酸酯
糠酸氟替卡松-[D3]
英文别名
AvaMys
Veramyst
AllerMist
Gw 685698x
GSK 685 698
Unii-js86977wnv
FLUTICASONE FUROATE
Fluticasone Foruate
Fluticasone Furoate-d3
Fluticasone Impurity 31 (Fluticasone Furoate)

物理化学性质

熔点250-252°C (dec.)
沸点625.2±55.0 °C(Predicted)
密度1.39
储存条件-20°C冷冻
溶解度可溶于氯仿(轻微、加热、超声处理)、甲醇(轻微)
酸度系数(pKa)12.52±0.70(Predicted)
形态固体
颜色白色至灰白色

安全数据

危险性符号(GHS)
GHS08
警示词警告
危险性描述H361d

常见问题列表

用途

糠酸氟替卡松为源自氟替卡松的一种人工合成皮质类固醇,可治疗过敏性鼻炎用。

生物活性

糠酸氟替卡松(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.

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