现货大促销,价格低至8折起,量大更优惠,详细咨询客服
全部分类
全部分类
  • Celecoxib
Celecoxib的可视化放大

Celecoxib

An NSAID and a COX-2 inhibitor

原价
¥637-637
价格
510-510
Celecoxib的二维码

所有产品仅用于科学研究,我们不为任何个人用途提供产品和服务

询价有惊喜,量大更优惠 点击这里给我发消息

  • 库存: 现货
可选包装 >>>
首页
  • 货号: ajci13192
  • CAS: 169590-42-5
  • 别名: 塞来昔布; SC 58635
  • 分子式: C17H14F3N3O2S
  • 分子量: 381.37
  • 纯度: >98%
  • 溶解度: ≥ 19.1mg/mL in DMSO
  • 储存: Store at -20°C
  • 库存: 现货

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].

参考文献:
[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.

Protocol

Kinase experiment [1]:

COX enzyme assay in vitro

Expression of COX protein in insect cells was determined by assessing PG-synthetic capability in homogenates from cells incubated for 3 days with COX-1 or COX-2 baculovirus. Cells expressing COX-1 or COX-2 were homogenized and incubated with arachidonic acid (10 μM). COX activity was determined by monitoring PG production. No COX activity was detected in mock-infected Sf9 cells. Celecoxib were preincubated with crude 1% CHAPS homogenates (2 ~ 10 μg of protein) for 10 mins before addition of arachidonic acid. PGE2 formed was detected by ELISA after 10 min incubation.

Cell experiment [2]:

Cell lines

A549 cells

Preparation method

The solubility of this compound in DMSO is > 19.1 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

0 ~ 10 μM

Applications

In A549 cells, Celecoxib (≤ 10 μM) and PGE2 (≤ 12.5 μM) showed no effect on cell viability. However, Celecoxib reversed PGE2 (10 μM) increased migration and invasion of A549 cells.

Animal experiment [2]:

Animal models

Mice received unilateral pneumonectomy

Dosage form

100 mg/kg; p.o.; q.d.

Applications

In mice received unilateral pneumonectomy, Celecoxib inhibited increased metastasis of A549 cells. Moreover, Celecoxib significantly inhibited the increase in PGE2 plasma level as well.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

参考文献:

[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.

动态评分

0.0

没有评分数据
没有评价数据
一键回到顶部
展开 收缩
安捷凯在线客服