Flurbiprofen(Synonyms: 氟比洛芬; dl-Flurbiprofen)

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Flurbiprofen (Synonyms: 氟比洛芬; dl-Flurbiprofen) 纯度: 99.85%

Flurbiprofen (dl-Flurbiprofen) 是一种高效的,具有口服活性的非甾体抗炎化合物,有退热止痛活性, 常用于炎症性疾病 (包括骨关节炎、类风湿关节炎) 的研究。Flurbiprofen 是一种非选择性的环氧合酶 (COX) 抑制剂,可用于结肠癌的研究。

Flurbiprofen(Synonyms: 氟比洛芬; dl-Flurbiprofen)

Flurbiprofen Chemical Structure

CAS No. : 5104-49-4

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生物活性

Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer[1][2][3].

IC50 & Target[1]

COX

 

COX-1

 

COX-2

 

体外研究
(In Vitro)

Flurbiprofen (2-20 nM; 12-48 hours) significantly decreases SW620 cells proliferation in a concentration- and time-dependent manner[1].
Flurbiprofen (10 nM; 24 hours) decreases COX-2 expression[1].
Flurbiprofen (10 nM; 24 hours) inhibits the expression of inflammatory factors by inhibiting COX-2[1].
Flurbiprofen (10 nM; 24 hours) promotes the apoptosis of colorectal cancer cells by inhibiting COX-2[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: SW620 cells
Concentration: 2 nM, 4 nM, 10 nM, 20 nM
Incubation Time: 12 hours, 24 hours, 48 hours
Result: Inhibited colorectal cancer cell proliferation.

Western Blot Analysis[1]

Cell Line: SW620 cells
Concentration: 10 nM
Incubation Time: 24 hours
Result: Significantly decreased the protein and mRNA levels of COX-2.

RT-PCR[1]

Cell Line: SW620 cells
Concentration: 10 nM
Incubation Time: 24 hours
Result: Decreased COX-2 mRNA expression levels

Apoptosis Analysis[1]

Cell Line: SW620 cells
Concentration: 10 nM
Incubation Time: 24 hours
Result: Significantly decreased the expression of Bcl2 and significantly increased the expression of Bax and cleaved-caspase3, with no effect on total caspase-3.

体内研究
(In Vivo)

Flurbiprofen (0.3-4.8 mg/kg; p.o.; 4-5 dosages) has acute anti-inflammatory in adrenalectomized rats[2].
Flurbiprofen (10 mg/kg; i.p.; daily; for 6 days) attenuates high-fat diet-induced obesity in mice[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rat[2]
Dosage: 0.3 mg/kg, 0.6 mg/kg, 1.2 mg/kg, 2.4 mg/kg, 4.8 mg/kg
Administration: Oral administration, 4-5 dosages
Result: Inhibited the acute inflammation.

Clinical Trial

分子量

244.26

Formula

C15H13FO2

CAS 号

5104-49-4

中文名称

氟比洛芬;氟联苯丙酸;苯氟布洛芬;氟苯布洛芬;氟布洛芬;氟吡洛芬

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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (409.40 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.0940 mL 20.4700 mL 40.9400 mL
5 mM 0.8188 mL 4.0940 mL 8.1880 mL
10 mM 0.4094 mL 2.0470 mL 4.0940 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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 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 (10.23 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.23 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% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (10.23 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.23 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

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

    Solubility: ≥ 2.5 mg/mL (10.23 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.23 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 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Xiaobo Wang, et al. Flurbiprofen suppresses the inflammation, proliferation, invasion and migration of colorectal cancer cells via COX2. Oncol Lett. 2020 Nov; 20(5): 132.

    [2]. E M Glenn, et al. The pharmacology of 2-(2-fluoro-4-biphenylyl)propionic acid (flurbiprofen). A potent non-steroidal anti-inflammatory drug. Agents Actions. 1973 Nov;3(4):210-6.

    [3]. Hosoi, T., et al., Flurbiprofen ameliorated obesity by attenuating leptin resistance induced by endoplasmic reticulum stress. EMBO Mol Med, 2014.

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