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Fluticasone Propionate

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Chemical Structure| 80474-14-2 同义名 : 丙酸氟替卡松 ;Fluticasone (propionate);Fluticasone 17-Propionate;Fluticasone Propionate, Cutivate, Flixonase, Flixotide, Flonase, Flovent;CCI-187881
CAS号 : 80474-14-2
货号 : A558252
分子式 : C25H31F3O5S
纯度 : 99+%
分子量 : 500.571
MDL号 : MFCD00866007
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(209.76 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Fluticasone propionate is a new corticosteroid based on the androstane nucleus. It is more lipophilic than beclomethasone dipropionate (BDP) and budesonide, and binds more avidly to human lung tissue. It has an absolute affinity (KD) of 0.5 nM for the glucocorticoid receptor and a relative receptor affinity 1.5- and 3.0-times greater than that of beclomethasone-17-monopropionate (17-BMP) and budesonide, respectively. The rate of association with the receptor is faster and the rate of dissociation slower than with standard corticosteroids. Pretreatment with fluticasone propionate significantly inhibits the increase in mast cell numbers in the nasal mucosa of rats chronically exposed to toluene di-isocyanate (TDI), and suppresses TDI-induced mast cell degranulation. Fluticasone propionate therefore has increased intrinsic glucocorticoid potency and high topical anti-inflammatory activity[3]. Fluticasone propionate is a potent topical anti-inflammatory corticosteroid with low systemic activity. Fluticasone propionate generally demonstrated similar efficacy compared with intranasal beclomethasone dipropionate, flunisolide acetonide and oral astemizole and better or a trend towards better efficacy compared with oral loratadine, terfenadine, cetirizine and intranasal sodium cromoglycate (cromolyn sodium) against nasal symptoms[4]. Inhaled fluticasone propionate < or =500 microg/day is an effective anti-inflammatory therapy for mild to moderate asthma in adolescents and adults[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01381471 - Completed - -
NCT01381471 - Completed - -
NCT01431924 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.00mL

0.40mL

0.20mL

9.99mL

2.00mL

1.00mL

19.98mL

4.00mL

2.00mL
参考文献

[1]Papi A, Price D, et al. Efficacy of fluticasone propionate/formoterol fumarate in the treatment of asthma: a pooled analysis. Respir Med. 2015 Feb;109(2):208-17.

[2]Muley P, Shah M, et al. Safety of inhaled fluticasone propionate therapy for pediatric asthma - a systematic review. Curr Drug Saf. 2013 Jul;8(3):186-94.

[3]Johnson M. The anti-inflammatory profile of fluticasone propionate. Allergy. 1995;50(23 Suppl):11-4

[4]Bryson HM, Faulds D. Intranasal fluticasone propionate. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in allergic rhinitis. Drugs. 1992 May;43(5):760-75.

[5]Jarvis B, Faulds D. Inhaled fluticasone propionate: a review of its therapeutic efficacy at dosages < or = 500 microg/day in adults and adolescents with mild to moderate asthma. Drugs. 1999 May;57(5):769-803