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Purity: ≥98%
Valdecoxib (SC-65872; SC65872; SC 65872; Bextra), a nonsteroidal anti-inflammatory drug (NSAID), is a potent and selective inhibitor of COX-2 enzyme with potential anti-inflammatory activity. It inhibits COX-2 with an IC50 of 5 nM. Valdecoxib has been approved for the treatment of pain and inflammation. Valdecoxib and its intravenous prodrug parecoxib exert significant opioid-sparing effects after dental, gynecologic, orthopedic and other noncardiac surgical procedures. In the cellular assay, valdecoxib shows inhibitory activity on human recombinant COX-2 with IC50 value of 5nM. It shows no significant effect on COX-1 with IC50 value of 140μM. In the ex vivo assay using human whole blood, valdecoxib prevents PGE2 production with IC50 value of 0.89μM.
| ln Vitro |
Compound 2, valdecoxib, is a very strong, specific, and oral active inhibitor of COX-2, having IC50 values of 140 μM for COX-1 and 5 nM for COX-2, respectively[1]. In a dose-dependent manner, valdecoxib (10, 100 μM) suppresses the proliferation of endothelial cells caused by LPS and the release of bFGF. In inflammatory circumstances, valdecoxib promotes the production of VEGF via HMEC-1[2].
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| ln Vivo |
In an acute anti-inflammatory experiment (rat carrageenan foot pad edema; ED50 = 10.2 ± 1.4 mg/kg), valdecoxib (Compound 2) exhibits strong oral efficacy. With an ED50 of 0.032 ± 0.002 mg/kg/day, valdecoxib demonstrates persistent anti-inflammatory efficacy in the rat adjuvant arthritis model[1]. In chronically stressed mice, valdecoxib (10 mg/kg, ip) greatly reduces the behavioral and biochemical (oxidative damage) alterations[3].
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| References |
[1]. Talley JJ, et al. 4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2. J Med Chem. 2000 Mar 9;43(5):775-7.
[2]. Wiktorowska-Owczarek A. The effect of valdecoxib on the production of growth factors evoked by hypoxia and bacterial lipopolysaccharide in HMEC-1 cells. Adv Clin Exp Med. 2013 Nov-Dec;22(6):795-800. [3]. Kumar A, et al. Protective effects of selective and non-selective cyclooxygenase inhibitors in an animal model of chronic stress. Neurosci Bull. 2010 Feb;26(1):17-27 |
| Molecular Formula |
C16H14N2O3S
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| Molecular Weight |
314.36
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| CAS # |
181695-72-7
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| Related CAS # |
Valdecoxib-d3;1219794-90-7
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| SMILES |
S(C1C([H])=C([H])C(=C([H])C=1[H])C1=C(C([H])([H])[H])ON=C1C1C([H])=C([H])C([H])=C([H])C=1[H])(N([H])[H])(=O)=O
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.95 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.95 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 0.5% methylcellulose+0.2% Tween 80 : 19 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1811 mL | 15.9053 mL | 31.8107 mL | |
| 5 mM | 0.6362 mL | 3.1811 mL | 6.3621 mL | |
| 10 mM | 0.3181 mL | 1.5905 mL | 3.1811 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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