Fluticasone furoate (Synonyms: 糠酸氟替卡松)
目录号: PL04389 纯度: ≥99%
CAS No. :397864-44-7
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中文名称
Fluticasone furoate
中文别名
糠酸氟替卡松 GMP;糠酸氟替卡松;阿苏美特可湿性粉剂;氟替卡松糠酸酯;糠酸氟替卡松-D3;糠酸氟替卡松-D5
英文名称
Fluticasone furoate
英文别名
Androsta-1,4-diene-17-carbothioicacid, 6,9-difluoro-17-[(2-furanylcarbonyl)oxy]-11-hydroxy-16-methyl-3-oxo-,S-(fluoromethyl) ester, (6a,11b,16a,17a)-;Androsta-1,4-diene-17-carbothioicacid, 6,9-difluoro-17-[(2-furanylcarbonyl)oxy]-11-hydroxy-16-methyl-3-oxo-,S-(fluoromethyl) ;Fluticasone Furoate;Allermist;Avamys;GW 685698X
Cas No.
397864-44-7
分子式
C27H29O6F3S
分子量
538.58
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
Fluticasone furoate is a topical, intranasal, enhanced-affinity synthetic trifluorinated corticosteroid with a K d of 0.3 nM. Fluticasone furoate has potent anti-inflamatory and anti-asthmatic activity, and low systemic exposure. Fluticasone furoate has the potential for allergic rhinitis treatment.
性状
Solid
IC50 & Target[1][2]
Kd: 0.3 nM (Corticosteroid)
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (185.67 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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