糠酸氟替卡松

• 常用名: 糠酸氟替卡松
• 英文名: Fluticasone furoate
• CAS号: 397864-44-7
• 分子量: 538.576
• 密度: 1.4±0.1 g/cm3
• 沸点: 625.2±55.0 °C at 760 mmHg
• 分子式: C₂₇H₂₉F₃O₆S
• 熔点: N/A
• 闪点: 331.9±31.5 °C

糠酸氟替卡松用途

Fluticasone furoate 是一种局部,鼻内,增强亲和力的合成的三氟皮质类固醇,Kd 为 0.3 nM。Fluticasone furoate 具有有效的抗炎和抗哮喘活性,并且全身暴露率低。Fluticasone furoate 可用于过敏性鼻炎的研究。

糠酸氟替卡松名称

• 中文名: 糠酸氟替卡松
• 英文名: fluticasone furoate

糠酸氟替卡松生物活性

• 描述: Fluticasone furoate 是一种局部,鼻内,增强亲和力的合成的三氟皮质类固醇,Kd 为 0.3 nM。Fluticasone furoate 具有有效的抗炎和抗哮喘活性,并且全身暴露率低。Fluticasone furoate 可用于过敏性鼻炎的研究。
• 相关类别:
  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
• 靶点实验:

  Kd: 0.3 nM (Corticosteroid)[1]

• 体外研究: 糠酸氟替卡松以鼻喷雾剂的形式出现,作为微粉化糠酸氟替卡松的水悬浮液,通过计量喷雾泵对鼻粘膜进行局部给药[1]。氟替卡松在抑制肿瘤坏死因子合成和作用方面显示出巨大的潜力。呋喃酸氟替卡松也能有效地防止不同刺激对培养的人肺上皮细胞的损伤[1]。
• 体内研究: 氟替卡松在体外与血浆蛋白结合率为99.4%,其他研究表明,该药物具有广泛的一级代谢。蛋白质结合是高度相关的,因为只有未结合的游离药物才能在受体部位发挥作用。糠酸氟替卡松的清除主要是通过细胞色素P450同工酶(CYP)3A4在肝脏中水解,将药物转化为17β-羧酸代谢物(M10),显示出低糖皮质激素受体激动剂效力。氟替卡松(Fluticasone furonate)主要在粪便中排泄,在尿液中只有少量排泄[1]。
• 参考文献:

  [1]. Giavina-Bianchi P, et al. Fluticasone furoate nasal spray in the treatment of allergic rhinitis. Ther Clin Risk Manag. 2008 Apr;4(2):465-72.

  [2]. Alizadeh Z, et al. Asthma phenotypes and T-bet protein expression in cells treated with Fluticasone Furoate/Vilanterol. Pulm Pharmacol Ther. 2020 Feb;60:101886.

糠酸氟替卡松物理化学性质

• 密度: 1.4±0.1 g/cm3
• 沸点: 625.2±55.0 °C at 760 mmHg
• 分子式: C₂₇H₂₉F₃O₆S
• 分子量: 538.576
• 闪点: 331.9±31.5 °C
• 精确质量: 538.163696
• PSA: 119.11000
• LogP: 4.01
• InChIKey: XTULMSXFIHGYFS-VLSRWLAYSA-N
• SMILES: CC1CC2C3CC(F)C4=CC(=O)C=CC4(C)C3(F)C(O)CC2(C)C1(OC(=O)c1ccco1)C(=O)SCF
• 蒸汽压: 0.0±1.9 mmHg at 25°C
• 折射率: 1.584

糠酸氟替卡松靶点实验

查看更多实验

实验名称：Binding affinity towards rat Gabra1 in an in vitro assay with cellular components mea... 来源：ChEMBL 靶标：Gamma-aminobutyric acid receptor subunit alpha-1 External Id：CHEMBL5291800

实验名称：Agonist activity at GR in human SW1353 cells transfected with luciferase gene linked ... 来源：ChEMBL 靶标：Glucocorticoid receptor External Id：CHEMBL1838801

实验名称：Binding affinity towards human GCGR in an in vitro assay with cellular components mea... 来源：ChEMBL 靶标：Glucagon receptor External Id：CHEMBL5291802

实验名称：Compound was evaluated for inhibition of rat Gabra1 in an in vitro assay with cellula... 来源：ChEMBL 靶标：Gamma-aminobutyric acid receptor subunit alpha-1 External Id：CHEMBL5291801

实验名称：Inhibition of TNFalpha release in human PBMC by ELISA assay 来源：ChEMBL 靶标：PBMC External Id：CHEMBL1838802

实验名称：Binding affinity towards human GABBR1 in an in vitro assay with cellular components m... 来源：ChEMBL 靶标：Gamma-aminobutyric acid type B receptor subunit 1 External Id：CHEMBL5291795

实验名称：Binding affinity towards rat Gabra1 in an in vitro assay with cellular components mea... 来源：ChEMBL 靶标：Gamma-aminobutyric acid receptor subunit alpha-1 External Id：CHEMBL5291798

实验名称：Binding affinity towards human ESR1 in an in vitro cell free assay (CRO assay) measur... 来源：ChEMBL 靶标：Estrogen receptor External Id：CHEMBL5291792

实验名称：Binding affinity towards human ESR1 in an in vitro cell free assay (NIBR assay) measu... 来源：ChEMBL 靶标：Estrogen receptor External Id：CHEMBL5291791

实验名称：Compound was evaluated for inhibition of human F2 in an in vitro cell free assay meas... 来源：ChEMBL 靶标：Prothrombin External Id：CHEMBL5291794

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糠酸氟替卡松英文别名

• 2-Furancarboxylic acid, (6α,11β,16α,17α)-6,9-difluoro-17-[[(fluoromethyl)thio]carbonyl]-11-hydroxy-16-methyl-3-oxoandrosta-1,4-dien-17-yl ester
• Ennhale
• Fluticasone furoate
• Furamist
• Veramyst
• (6α,11β,16α,17α)-6,9-Difluoro-17-{[(fluoromethyl)sulfanyl]carbonyl}-11-hydroxy-16-methyl-3-oxoandrosta-1,4-dien-17-yl 2-furoate
• Avamys