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397864-44-7

中文名稱 糠酸氟替卡松
英文名稱 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 2024/10/29 11:31:16
397864-44-7 結(jié)構(gòu)式 397864-44-7 結(jié)構(gòu)式

基本信息

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

物理化學(xué)性質(zhì)

熔點(diǎn)250-252°C (dec.)
沸點(diǎn)625.2±55.0 °C(Predicted)
密度1.39
儲(chǔ)存條件-20°C冷凍
溶解度可溶于氯仿(輕微、加熱、超聲處理)、甲醇(輕微)
酸度系數(shù)(pKa)12.52±0.70(Predicted)
形態(tài)固體
顏色白色至灰白色

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS08
警示詞警告
危險(xiǎn)性描述H361d

常見(jiàn)問(wèn)題列表

用途

糠酸氟替卡松為源自氟替卡松的一種人工合成皮質(zhì)類固醇,可治療過(guò)敏性鼻炎用。

生物活性

糠酸氟替卡松(GW685698)是一種吸入性皮質(zhì)類固醇/長(zhǎng)效的β腎上腺素能受體激動(dòng)劑的復(fù)方治療藥物,能延長(zhǎng)支氣管擴(kuò)張劑的作用時(shí)間。它被用于非過(guò)敏性和過(guò)敏性皮炎的治療。

靶點(diǎn)

Kd: 0.3 nM (Corticosteroid)

體外研究

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.

體內(nèi)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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