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