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Celecoxib

现货
Catalog No.
A1664
COX-2选择性抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 600.00
现货
100mg
¥ 600.00
现货

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Background

Celecoxib is a highly selective inhibitor of cyclooxygenase-2 (COX-2) with IC50 value of 40nM [1].

In vitro, celecoxib not only reduced the production of PGE2 but also inhibited the downstream effects of PGE2. Celecoxib blocked migration and invasion of A549 cells increased by PGE2 in the wound healing and transwell assays.  Additionally, celecoxib reduced MMP9 mRNA expression which was increased by PGE2. Moreover, celecoxib enhanced E-cadherin mRNA expression which was inhibited by PGE2 [2].

In vivo, celecoxib inhibited the increase in metastases of A549 cells and significantly reduced the increase in PGE2 plasma level in mice receiving unilateral pneumonectomy [2].

References:
[1] Penning TD1, Talley JJ, Bertenshaw SR, Carter JS, Collins PW, Docter S, Graneto MJ, Lee LF, Malecha JW, Miyashiro JM, Rogers RS, Rogier DJ, Yu SS,AndersonGD, Burton EG, Cogburn JN, Gregory SA, Koboldt CM, Perkins WE, Seibert K, Veenhuizen AW, Zhang YY, Isakson PC. Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib). J Med Chem. 1997 Apr 25;40(9):1347-65.
[2] Zhang S1, Da L1, Yang X1, Feng D1, Yin R1, Li M1, Zhang Z1, Jiang F2, Xu L3. Celecoxib potentially inhibits metastasis of lung cancer promoted by surgery in mice, via suppression of the PGE2-modulated β-catenin pathway.

Toxicol Lett. 2014 Mar 3;225(2):201-7.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt381.37
Cas No.169590-42-5
FormulaC17H14F3N3O2S
Solubility≥19.1mg/mL in DMSO
Chemical Name4-[5-(4-methylphenyl)-3-(trifluoromethyl)pyrazol-1-yl]benzenesulfonamide
SDFDownload SDF
Canonical SMILESCC1=CC=C(C=C1)C2=CC(=NN2C3=CC=C(C=C3)S(=O)(=O)N)C(F)(F)F
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

激酶实验 [1]:

体外COX酶实验

将细胞与COX-1或COX-2杆状病毒温育3天,捣碎细胞,通过评估基于细胞匀浆的PG合成能力,测定昆虫细胞COX蛋白表达量。将含COX-1或COX-2的细胞匀浆与花生四烯酸 (10 μM) 混合。通过PG产量评估COX活性。在模拟感染的Sf9细胞中,检测不出COX活性。将Celecoxib与天然的1% CHAPS匀浆(2 ~ 10 μg蛋白)预温育10分钟,然后加入花生四烯酸。温育10分钟后,通过ELISA检测形成的PGE2。

细胞实验 [2]:

细胞系

A549细胞

制备方法

在DMSO中的溶解度大于19.1 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

0 ~ 10 μM

实验结果

在A549细胞中,Celecoxib (≤ 10 μM) 和PGE2 (≤ 12.5 μM) 对细胞活力没有影响。然而,Celecoxib逆转PGE2 (10 μM) 诱导的A549细胞迁移和侵袭。

动物实验 [2]:

动物模型

接受单侧肺切除术的小鼠

给药剂量

100 mg/kg;口服给药;每日1次

实验结果

在接受单侧肺切除术的小鼠中,Celecoxib抑制A549细胞转移的增加。此外,Celecoxib同时还显著抑制PGE2血浆水平的增加。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Penning TD1, Talley JJ, Bertenshaw SR, Carter JS, Collins PW, Docter S, Graneto MJ, Lee LF, Malecha JW, Miyashiro JM, Rogers RS, Rogier DJ, Yu SS,AndersonGD, Burton EG, Cogburn JN, Gregory SA, Koboldt CM, Perkins WE, Seibert K, Veenhuizen AW, Zhang YY, Isakson PC. Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib). J Med Chem. 1997 Apr 25;40(9):1347-65.

[2]. Zhang S1, Da L1, Yang X1, Feng D1, Yin R1, Li M1, Zhang Z1, Jiang F2, Xu L3. Celecoxib potentially inhibits metastasis of lung cancer promoted by surgery in mice, via suppression of the PGE2-modulated β-catenin pathway. Toxicol Lett. 2014 Mar 3;225(2):201-7.

质量控制

化学结构

Celecoxib