90566-53-3

• 常用中文名：氟替卡松
• 常用英文名：Fluticasone
• CAS号：90566-53-3
• 分子式：C₂₅H₃₁F₃O₅S
• 分子量：500.571
• 相关类别： 原料药 激素及调节内分泌功能类药 肾上腺皮质激素类药
• 发布时间：2018-08-07 11:35:08
• 更新时间：2024-01-02 19:47:22
• 氟替卡松是一种用于呼吸系统疾病的吸入性皮质类固醇[1]。氟替卡松是一种Smo激动剂,IC50值为99 nM。氟替卡松激活刺猬信号并促进原代神经干/前体细胞的增殖[2]。

名称

• 中文名: 氟替卡松
• 英文名: fluticasone
• 英文别名: Fluticasone propionate (JAN/USAN); Flonase; Androsta-1,4-diene-17-carbothioic acid, 6,9-difluoro-11-hydroxy-16-methyl-3-oxo-17-(1-oxopropoxy)-, S-(fluoromethyl) ester, (6α,11β,16α,17α)-; S-(fluoromethyl) (6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-difluoro-11,17-dihydroxy-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthrene-17-carbothioate; Flovent DPI; UNII-CUT2W21N7U; Flixonase; Flutionum; Flutiona [Spanish]; (6α,11β,16α,17α)-6,9-Difluoro-17-{[(fluoromethyl)sulfanyl]carbonyl}-11-hydroxy-16-methyl-3-oxoandrosta-1,4-dien-17-yl propionate; Flixotide; Fluticasone; Fluticasone propionate; Flutiona; flutione; Fluticaps (TN); (6α,11β,16α,17α)-6,9-difluoro-17-{[(fluoromethyl)sulfanyl]carbonyl}-11-hydroxy-16-methyl-3-oxoandrosta-1,4-dien-17-yl propanoate; (6a,11b,16a,17a)-6,9-Difluoro-11-hydroxy-16-methyl-3-oxo-17-(1-oxopropoxy)androsta-1,4-diene-17-carbothioic Acid S-(Fluoromethyl) Ester; flovent diskus; Flutionum [Latin]; Flutione (INN); Cutivate; MFCD01862254

物化性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 568.3±50.0 °C at 760 mmHg
• 熔点: -18.1ºC
• 分子式: C₂₅H₃₁F₃O₅S
• 分子量: 500.571
• 闪点: 297.5±30.1 °C
• 精确质量: 500.184418
• PSA: 105.97000
• LogP: 3.73
• 蒸汽压: 0.0±3.5 mmHg at 25°C
• 折射率: 1.556

生物活性

• 描述: 氟替卡松是一种用于呼吸系统疾病的吸入性皮质类固醇[1]。氟替卡松是一种Smo激动剂,IC50值为99 nM。氟替卡松激活刺猬信号并促进原代神经干/前体细胞的增殖[2]。
• 相关类别:
  信号通路 >> 干细胞及 Wnt 通路 >> SMO
  研究领域 >> 内分泌
  研究领域 >> 感染
  研究领域 >> 炎症/免疫
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 糖皮质激素受体
• 体外研究: 氟替卡松(0-10μM,2小时)抑制U2OS细胞生长,EC50为99 nM[2]。氟替卡松(10-1000 nM,48小时)减少HRV诱导的粘蛋白产生,并涉及SPDEF调节基因和细胞外ATP释放的调节[3]。
• 体内研究: 氟替卡松(经鼻滴注；1mg/kg；7天)抑制鼻病毒诱导的体内气道炎症,但也损害抗病毒免疫反应,增加病毒滴度,导致粘液高分泌[4]。动物模型：C57BL/6小鼠[4]剂量：1mg/kg给药：滴鼻；感染鼻病毒1B前1小时；7天结果：抑制BAL中性粒细胞数量,抑制鼻病毒诱导的气道炎症。
• 参考文献:

  [1]. Seidel P, et al. Thiazolidinediones inhibit airway smooth muscle release of the chemokine CXCL10: in vitro comparison with current asthma therapies. Respir Res. 2012 Oct 4. 13(1):90.

  [2]. Wang J, et al. Identification of select glucocorticoids as Smoothened agonists: potential utility for regenerative medicine. Proc Natl Acad Sci U S A. 2010 May 18. 107(20):9323-8.

  [3]. Ying Wang, et al. Tiotropium and Fluticasone Inhibit Rhinovirus-Induced Mucin Production via Multiple Mechanisms in Differentiated Airway Epithelial Cells. Front. Cell. Infect. Microbiol., 2020 Jun.

  [4]. Singanayagam A, et al. Effect of fluticasone propionate on virus-induced airways inflammation and anti-viral immune responses in mice. Lancet. 2015 Feb 26. 385(Suppl 1):S88.