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Fluticasone furoate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Fluticasone furoate图片
CAS NO:397864-44-7
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
10mg电议
50mg电议
100mg电议

产品名称
糠酸氟替卡松
产品介绍
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 trifluorinatedcorticosteroidwith aKdof 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[1][2].

IC50& Target

Kd: 0.3 nM (Corticosteroid)[1]

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[1].
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[1].

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[1].

Clinical Trial
分子量

538.58

性状

Solid

Formula

C27H29F3O6S

CAS 号

397864-44-7

中文名称

糠酸氟替卡松

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL(185.67 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.8567 mL9.2837 mL18.5673 mL
5 mM0.3713 mL1.8567 mL3.7135 mL
10 mM0.1857 mL0.9284 mL1.8567 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (4.64 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.64 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (4.64 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.64 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。