Ibuprofen (Synonyms: DL-Ibuprofen, NSC 256857, U-18753) |
| Catalog No.GC17863 |
inhibitor of cyclooxygenase 1 and cyclooxygenase 2
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 15687-27-1
Sample solution is provided at 25 µL, 10mM.
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Ibuprofen is an inhibitor of cyclooxygenase 1 and cyclooxygenase 2 with IC50 values of 12 and 80 μM, respectively [1].
Cyclooxygenase (COX) is an enzyme that is responsible for the formation of prostaglandins, prostacyclin and thromboxane.
In HCT-116 p53wt or HCT-116 p53-/-colon carcinoma cell lines, S- and R-ibuprofen induced apoptosis and blocked cell cycle is in part dependent on p53. The anti-proliferative effects were significantly higher in the p53wt cell line than in the p53-deficient cells [2].
In nude mice model bearing HCT-116 p53wt and p53-/- xenografts, R-ibuprofen significantly inhibited the growth of p53wt expressing xenografts and only a small inhibition of p53-/- xenografts [2]. In hypercholesterolemic animals, ibuprofen reduced the levels of total cholesterol, VLDL, LDL, triglycerides and atherogenic index. Also, ibuprofen inhibited COX enzymes and inhibited the generation of free radicals during prostaglandins synthesis, which reduced the levels of lipid peroxidation, superoxide dismutase [3]. In rats, ibuprofen (60 mg/kg) improved mechanical hyperalgesia through reducing central hyperexcitability [4].
References:
[1]. Kato M, Nishida S, Kitasato H, et al. Cyclooxygenase-1 and cyclooxygenase-2 selectivity of non-steroidal anti-inflammatory drugs: investigation using human peripheral monocytes. J Pharm Pharmacol, 2001, 53(12): 1679-1685.
[2]. Janssen A, Schiffmann S, Birod K, et al. p53 is important for the anti-proliferative effect of ibuprofen in colon carcinoma cells. Biochem Biophys Res Commun, 2008, 365(4): 698-703.
[3]. Dabhi JK, Solanki JK, Mehta A. Antiatherosclerotic activity of ibuprofen, a non-selective COX inhibitor--an animal study. Indian J Exp Biol, 2008, 46(6): 476-481.
[4]. Redondo-Castro E, Navarro X. Chronic ibuprofen administration reduces neuropathic pain but does not exert neuroprotection after spinal cord injury in adult rats. Exp Neurol, 2014, 252: 95-103.
| Cell experiment [1]: | |
|
Cell lines |
p53 wild-type or p53-deficient human colon cancer HCT-116 cell lines |
|
Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
0-1000 μM; 24 h (cell cycle distribution) or 72 h (apoptosis). |
|
Applications |
In a colony forming assay, S-ibuprofen and R-ibuprofen exhibited significantly higher anti-proliferative effects in the p53wt cell line than in the p53-deficient HCT-116 cells. In HCT-116 p53wt cells, 800-1000 μM S-ibuprofen and R-ibuprofen reduced cells in the S and G2/M phases and significantly increased the number of cells in the G0/G1-phase. 800-1000 μM S- and R-ibuprofen also significantly increased apoptosis. |
| Animal experiment [1]: | |
|
Animal models |
Athymic nude mice xenografted with implanted subcutaneously with HCT-116 p53wt and p53-/- colon cancer cells |
|
Dosage form |
five days a week intraperitoneally with 15 mg/kg/day, suspended in PBS (pH 7), 5 weeks |
|
Application |
Compared with the tumour volumes of untreated mice, R-ibuprofen significantly reduced the growth of p53wt expressing xenografts. S-ibuprofen also reduced the growth of p53wt expressing xenografts. But only a small and non-significant inhibition of HCT-116 p53-/- tumour growth after S- or R-ibuprofen treatment. |
|
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]. Janssen A, Schiffmann S, Birod K, et al. p53 is important for the anti-proliferative effect of ibuprofen in colon carcinoma cells. Biochem Biophys Res Commun, 2008, 365(4): 698-703. |
|
| Cas No. | 15687-27-1 | SDF | |
| Synonyms | DL-Ibuprofen, NSC 256857, U-18753 | ||
| Chemical Name | 2-[4-(2-methylpropyl)phenyl]propanoic acid | ||
| Canonical SMILES | CC(C)CC1=CC=C(C=C1)C(C)C(=O)O | ||
| Formula | C13H18O2 | M.Wt | 206.28 |
| Solubility | ≥ 10.3mg/mL in DMSO | Storage | Store at RT |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.8478 mL | 24.2389 mL | 48.4778 mL |
| 5 mM | 0.9696 mL | 4.8478 mL | 9.6956 mL |
| 10 mM | 0.4848 mL | 2.4239 mL | 4.8478 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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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.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)
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