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/ Fluticasone Propionate/氟替卡松丙酸酯

Fluticasone Propionate/氟替卡松丙酸酯 {[allProObj[0].p_purity_real_show]}

货号：A558252 同义名： 丙酸氟替卡松 / Fluticasone (propionate); Fluticasone 17-Propionate

Fluticasone Propionate 是一种高亲和力的糖皮质激素受体激动剂（KD = 0.5 nM），几乎不与其他甾体受体结合，常用于过敏性鼻炎、哮喘等炎症机制研究。

Fluticasone Propionate/氟替卡松丙酸酯 化学结构 CAS号：80474-14-2
Fluticasone Propionate/氟替卡松丙酸酯 化学结构
CAS号：80474-14-2
Fluticasone Propionate/氟替卡松丙酸酯 3D分子结构
CAS号：80474-14-2
Fluticasone Propionate/氟替卡松丙酸酯 化学结构 CAS号：80474-14-2
Fluticasone Propionate/氟替卡松丙酸酯 3D分子结构 CAS号：80474-14-2
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Fluticasone Propionate/氟替卡松丙酸酯 纯度/质量文件 产品仅供科研

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Fluticasone Propionate/氟替卡松丙酸酯 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].

Fluticasone Propionate/氟替卡松丙酸酯 细胞实验

Cell Line
Concentration Treated Time Description References
Airway epithelial cells from COPD patients 1 and 10 nM 48 hours To evaluate the inhibitory effect of FP on RV-induced IFNβ, IFNλ1, and IFNλ2/3 mRNA expression Nat Commun. 2018 Jun 8;9(1):2229.
BEAS-2B cells 1 and 10 nM 24 hours To evaluate the inhibitory effect of FP on RV-induced IFNβ and IFNλ2/3 mRNA expression Nat Commun. 2018 Jun 8;9(1):2229.
Primary bronchial epithelial cells from COPD patients 10 nM 8 hours To evaluate the effect of fluticasone propionate on hCAP18/LL-37 production in primary bronchial epithelial cells from COPD patients. Results showed that fluticasone propionate treatment significantly reduced hCAP18/LL-37 production. Sci Transl Med. 2019 Aug 28;11(507):eaav3879.
BEAS-2B bronchial epithelial cells 1 or 10 nM 8 hours To evaluate the effect of fluticasone propionate on hCAP18/LL-37 production after S. pneumoniae infection. Results showed that fluticasone propionate treatment significantly reduced hCAP18/LL-37 production. Sci Transl Med. 2019 Aug 28;11(507):eaav3879.
Human bronchial airway epithelial cells (BAEC-ALI) 10^-7 M 24 hours Induced expression and secretion of FGF1, FGF2, FGF4, and FGF18 Sci Transl Med. 2022 Apr 20;14(641):eabl8146.
BEAS2B bronchial epithelial cells 0.1-1,000 nM 24 hours Assess the effects of ICS on bacterial burden. FP and budesonide increased bacterial loads at concentrations of 1 nM or higher, while BDP only showed significant effects at the highest concentration (1,000 nM). Chest. 2020 Sep;158(3):947-951.
BEAS2B bronchial epithelial cells 0.1-1,000 nM 1 hour Evaluate the anti-inflammatory effects of FP, budesonide, and BDP during S. pneumoniae infection. FP and budesonide significantly suppressed IL-6 and IL-8 induction at concentrations of 1 nM and higher, while BDP only had significant effects at 10 nM or higher. Chest. 2020 Sep;158(3):947-951.
FoxP3-GFP mouse splenic regulatory T cells (Tregs) 3 nM 16 hours Tregs were resistant to FLU-induced apoptosis with only 10% viability reduction, leading to increased Treg:Tconv ratio EMBO Mol Med. 2023 Sep 11;15(9):e17748.
Murine bone marrow hematopoietic stem cells 3 nM 16 hours FLU significantly upregulated CXCR4 expression on HSCs, enhanced HSC migration capacity, and improved bone marrow engraftment efficiency EMBO Mol Med. 2023 Sep 11;15(9):e17748.

Fluticasone Propionate/氟替卡松丙酸酯 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Elastase-induced COPD model Intranasal administration 20 μg Single dose, evaluated at 8 hours post-infection To evaluate the effect of fluticasone propionate on bacterial clearance in the lungs after S. pneumoniae infection. Results showed that fluticasone propionate treatment significantly increased lung bacterial loads and suppressed cathelicidin production. Sci Transl Med. 2019 Aug 28;11(507):eaav3879.
Mice HDM-induced airway inflammation model Intratracheal administration 1 mg/kg Administered on days 14, 16, 18, 28, and 30 Inhibited type 2 cytokine responses and airway eosinophilia while concomitantly inducing FGFs and enhancing airway neutrophilia Sci Transl Med. 2022 Apr 20;14(641):eabl8146.
C57BL/6 mice RV infection model Intranasal administration 20 μg Single dose To evaluate the effect of FP on innate and adaptive immune responses to RV infection, results showed FP suppressed IFN responses, delayed virus clearance, and increased mucus production and bacterial loads Nat Commun. 2018 Jun 8;9(1):2229.
C57BL/6 mice S. pneumoniae infection model Intranasal administration 20 mg Single dose Evaluate the effects of ICS on inflammation and antibacterial immunity in vivo. FP and budesonide significantly suppressed IL-6, TNF, IL-1β, and CXCL2/MIP-2 induction and reduced airway neutrophil recruitment. FP and budesonide also increased lung bacterial loads and reduced induction of the cathelicidin-related AMP (CRAMP), while BDP had no significant effects. Chest. 2020 Sep;158(3):947-951.
Mice B6→Balb/c allogeneic hematopoietic cell transplantation model IV transplantation after ex vivo pre-treatment 3 nM Single 16-hour pre-treatment before transplantation FLU pre-treatment significantly reduced aGvHD severity and mortality, increased regulatory T cell ratio while maintaining hematopoietic stem cell engraftment capacity EMBO Mol Med. 2023 Sep 11;15(9):e17748.

Fluticasone Propionate/氟替卡松丙酸酯 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 - -

Fluticasone Propionate/氟替卡松丙酸酯 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

Fluticasone Propionate/氟替卡松丙酸酯 实验方案

计算器
存储液制备 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

Fluticasone Propionate/氟替卡松丙酸酯 技术信息

CAS号80474-14-2
分子式C25H31F3O5S
分子量 500.57
SMILES Code O=C(CC)O[C@@]([C@]([C@@]1([H])C2)(C[C@H](O)[C@](F)([C@]3(C=C4)C)[C@@]1([H])C[C@H](F)C3=CC4=O)C)([C@@H]2C)C(SCF)=O
MDL No. MFCD00866007
别名 丙酸氟替卡松 ;Fluticasone (propionate); Fluticasone 17-Propionate; Fluticasone Propionate, Cutivate, Flixonase, Flixotide, Flonase, Flovent; CCI-187881
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一

Tags: Fluticasone (propionate) | 80474-14-2 | Glucocorticoid Receptor | Enterovirus | Glucocorticoid Receptor Agonist | Immunology/Inflammation | Vitamin D Related/Nuclear Receptor | Anti-infection | Metabolic Enzyme/Protease | Glucocorticoid Receptor | Enterovirus | Endogenous Metabolite | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Fluticasone Propionate/氟替卡松丙酸酯 纯度/质量文件 | Fluticasone Propionate/氟替卡松丙酸酯 生物活性 | Fluticasone Propionate/氟替卡松丙酸酯 临床数据 | Fluticasone Propionate/氟替卡松丙酸酯 参考文献 | Fluticasone Propionate/氟替卡松丙酸酯 实验方案 | Fluticasone Propionate/氟替卡松丙酸酯 技术信息

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