Celecoxib (Synonyms: SC58635, YM177) |
Catalog No.GC14475 |
Selective cyclooxygenase-2 (COX-2) inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 169590-42-5
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. |
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. |
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.
Cas No. | 169590-42-5 | SDF | |
Synonyms | SC58635, YM177 | ||
Chemical Name | 4-[5-(4-methylphenyl)-3-(trifluoromethyl)pyrazol-1-yl]benzenesulfonamide | ||
Canonical SMILES | CC1=CC=C(C=C1)C2=CC(=NN2C3=CC=C(C=C3)S(=O)(=O)N)C(F)(F)F | ||
Formula | C17H14F3N3O2S | M.Wt | 381.37 |
Solubility | ≥ 19.1mg/mL in DMSO | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.6221 mL | 13.1106 mL | 26.2213 mL |
5 mM | 0.5244 mL | 2.6221 mL | 5.2443 mL |
10 mM | 0.2622 mL | 1.3111 mL | 2.6221 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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