| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Parecoxib (SC69124A; Dynastat) is a selective cyclooxygenase-2 (COX-2) inhibitor with the potential for treating postoperative pain in adults. It is a water-soluble and injectable prodrug of valdecoxib.
| ln Vitro |
Parecoxib (0-200 μM; 24-48 hours) reduces the growth of GBM cells in a dose-dependent manner [4]. Parecoxib (200 μM; 24-48 hours) caused the migratory ability of U343 cells to be reduced compared with the PBS-treated group [4].
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| ln Vivo |
In the elevated plus maze test, parecoxib (ip; 2.5, 5.0, or 10 mg/kg; once daily; 21 days) had no effect on locomotor activity; however, the percentage of time spent with arms outstretched was higher for parecoxib at doses of 5 and 10 mg/kg[3].
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| Cell Assay |
Cell Viability Assay [4]
Cell Types: GBM Cells: U251 and U343 Cell Tested Concentrations: 0 μM, 20 μM, 50 μM, 100 μM and 200 μM Incubation Duration: 24-48 hrs (hours) Experimental Results: Result in slower BrdU incorporation into GBM Cells include U251 and U343 cells. |
| Animal Protocol |
Animal/Disease Models: Adult male ICR mouse, 15 weeks old, weighing 25-35 grams [3]
Doses: 2.5, 5.0 or 10 mg/kg Route of Administration: intraperitoneal (ip) injection; 2.5, 5.0 or 10 mg/kg; one time/day; 21-day Experimental Results: Anxiolytic-like effects in the elevated plus maze test |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Hepatic. Metabolized primarily via CYP3A4 and 2C9 to valdecoxib and propionic acid. Biological Half-Life 22 minutes (parecoxib); 8 hours (valdecoxib) |
| Toxicity/Toxicokinetics |
Protein Binding
98% |
| References |
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| Additional Infomation |
Parecoxib is an N-acylsulfonamide resulting from the formal condensation of valdecoxib with propionic acid. It is a prodrug for valdecoxib. It has a role as a cyclooxygenase 2 inhibitor, a non-narcotic analgesic, a non-steroidal anti-inflammatory drug and a prodrug. It is a member of isoxazoles and a N-sulfonylcarboxamide. It is functionally related to a valdecoxib.
Parecoxib is a water-soluble and injectable prodrug of valdecoxib. It is marketed as Dynastat in the European Union. Parecoxib is a COX2 selective inhibitor in the same category as celecoxib (Celebrex) and rofecoxib (Vioxx). As it is injectable, it can be used perioperatively when patients are unable to take oral medications. It is approved through much of Europe for short term perioperative pain control much in the same way ketorolac (Toradol) is used in the United States. A letter of non-approval for parecoxib was issued by the FDA in 2005. Parecoxib is an amide prodrug of the cyclooxygenase II (COX-2) selective, non-steroidal anti-inflammatory drug (NSAID) valdecoxib, with anti-inflammatory, analgesic, and antipyretic activities. Upon administration, parecoxib is hydrolyzed by hepatic carboxyesterases to its active form, valdecoxib. Valdecoxib selectively binds to and inhibits COX-2. This prevents the conversion of arachidonic acid into prostaglandins, which are involved in the regulation of pain, inflammation, and fever. This NSAID does not inhibit COX-1 at therapeutic concentrations and, therefore, does not interfere with blood coagulation. Drug Indication Used for short term perioperative pain control. For the short-term treatment of postoperative pain in adults. , For the short-term treatment of postoperative pain. The decision to prescribe a selective COX-2 inhibitor should be based on an assessment of theindividual patient's overall risks (see sections 4. 3, 4. 4). For the short-term treatment of postoperative pain. |
| Molecular Formula |
C19H18N2O4S
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|---|---|
| Molecular Weight |
370.42222
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| Exact Mass |
370.098
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| CAS # |
198470-84-7
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| Related CAS # |
Parecoxib Sodium;198470-85-8;Parecoxib-d3
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| PubChem CID |
119828
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Melting Point |
148.9-151°
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| Index of Refraction |
1.580
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| LogP |
1.72
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
26
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| Complexity |
575
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
TZRHLKRLEZJVIJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H18N2O4S/c1-3-17(22)21-26(23,24)16-11-9-14(10-12-16)18-13(2)25-20-19(18)15-7-5-4-6-8-15/h4-12H,3H2,1-2H3,(H,21,22)
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| Chemical Name |
N-[4-(5-methyl-3-phenyl-1,2-oxazol-4-yl)phenyl]sulfonylpropanamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO : ≥ 50 mg/mL (~134.98 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.75 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 (6.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6996 mL | 13.4982 mL | 26.9964 mL | |
| 5 mM | 0.5399 mL | 2.6996 mL | 5.3993 mL | |
| 10 mM | 0.2700 mL | 1.3498 mL | 2.6996 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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