| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Targets |
Parecoxib sodium is a prodrug that is converted to valdecoxib, its active metabolite. Valdecoxib is a selective inhibitor of the cyclooxygenase-2 (COX-2) enzyme. By inhibiting COX-2, it reduces the synthesis of prostaglandins, which are key mediators of inflammation and pain.
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| ln Vitro |
In a dose-dependent manner, parecoxib sodium (0-200 μM; 24-48 hours) suppresses the growth of GBM cells [4]. Parecoxib sodium (200 μM; 24-48 hours) decreased U343 cells' ability to migrate when compared to the PBS-treated group [4].
In vitro, Parecoxib sodium is converted to valdecoxib by human liver microsomes. Valdecoxib then acts as a potent and selective COX-2 inhibitor. Its COX-2 selectivity reduces the gastrointestinal side effects associated with non-selective NSAIDs. |
| ln Vivo |
In the elevated plus maze test, parecoxib sodium (ip; 2.5, 5.0, or 10 mg/kg; once daily; 21 days) had no effect on locomotor activity, but parecoxib 5 and 10 mg/kg was found to have a percentage greater level of motor activity. duration of open arms[3].
In vivo, Parecoxib sodium is converted to valdecoxib in rats, dogs, and cynomolgus monkeys. It is administered intravenously or intramuscularly for the management of postoperative pain. |
| Enzyme Assay |
The cell-free assay for COX-2 inhibition involves incubating the COX-2 enzyme with arachidonic acid and varying concentrations of the active metabolite, valdecoxib. The production of prostaglandin PGE2 is measured, typically by ELISA or mass spectrometry. The concentration required to inhibit 50% of enzyme activity (IC50) is calculated.
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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. Cellular assays for COX-2 inhibition use cell lines that express COX-2, such as macrophages stimulated with LPS. Cells are pre-treated with Parecoxib sodium or valdecoxib and then stimulated. The amount of PGE2 released into the culture medium is measured by ELISA to assess the compound's inhibitory effect. |
| Animal Protocol |
Animal/Disease Models: Adult male ICR mouse, 15 weeks old, weighing 25-35 grams [3]
Doses: 2.5 mg/kg, 5.0 mg/kg or 10 mg/kg Route of Administration: intraperitoneal (ip) injection; 2.5, 5.0 or 10 mg /kg; one time/day; 21 days Experimental Results: Exercised anxiolytic-like effects in the elevated plus maze test. In animal models, Parecoxib sodium is administered via injection. Efficacy is assessed in models of inflammation and pain, such as the carrageenan-induced paw edema model. Analgesic activity can be measured using the tail-flick or hot-plate tests. |
| ADME/Pharmacokinetics |
Parecoxib sodium is the prodrug of valdecoxib. It is water-soluble and rapidly converted to the active drug in vivo. Its half-life is short, making it suitable for acute pain management.
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| Toxicity/Toxicokinetics |
As a COX-2 inhibitor, Parecoxib sodium shares the toxicity profile of other drugs in this class. Potential risks include cardiovascular events, gastrointestinal bleeding (though lower than non-selective NSAIDs), and renal impairment. It is contraindicated in patients with a history of allergic reactions to sulfonamides.
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| References |
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| Additional Infomation |
Parecoxib sodium is the water-soluble injectable sodium salt form of parecoxib, an amide prodrug of vardicoxib, a cyclooxygenase II (COX-2) selective nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects. After intravenous or intramuscular injection, parecoxib is hydrolyzed by hepatic carboxylesterases to its active form, vardicoxib. Vardicoxib selectively binds to COX-2 and inhibits its activity. This prevents the conversion of arachidonic acid to 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 clotting. Indications: For short-term treatment of postoperative pain in adults. The decision to prescribe a selective COX-2 inhibitor should be based on an assessment of the overall risk to the individual patient (see Sections 4.3 and 4.4).
Parecoxib sodium is an FDA-approved drug used for the short-term management of postoperative pain. It is available as an injectable formulation. It was developed to provide the benefits of COX-2 inhibition with a rapid onset of action for acute pain. |
| Molecular Formula |
C19H17N2NAO4S
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|---|---|
| Molecular Weight |
392.4048
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| Exact Mass |
392.08
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| Elemental Analysis |
C, 58.16; H, 4.37; N, 7.14; Na, 5.86; O, 16.31; S, 8.17
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| CAS # |
198470-85-8
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| Related CAS # |
Parecoxib;198470-84-7;Parecoxib-d5 sodium
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| PubChem CID |
15895902
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| Appearance |
White to off-white solid powder
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| Boiling Point |
538ºC at 760mmHg
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| Melting Point |
273-275°C
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| Flash Point |
279.2ºC
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| LogP |
5.396
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
581
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| Defined Atom Stereocenter Count |
0
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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-]C(C([H])([H])C([H])([H])[H])=O)(=O)=O.[Na+]
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| InChi Key |
HQPVVKXJNZEAFW-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C19H18N2O4S.Na/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)/q+1/p-1
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| Chemical Name |
sodium ((4-(5-methyl-3-phenylisoxazol-4-yl)phenyl)sulfonyl)(propionyl)amide
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| Synonyms |
SC 69124A sodium SC-69124A Parecoxib sodiumSC69124A Dynastat
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ≥ 100 mg/mL (~254.84 mM)
H2O : ≥ 100 mg/mL (~254.84 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.37 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 (6.37 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 (6.37 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: 100 mg/mL (254.84 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5484 mL | 12.7421 mL | 25.4842 mL | |
| 5 mM | 0.5097 mL | 2.5484 mL | 5.0968 mL | |
| 10 mM | 0.2548 mL | 1.2742 mL | 2.5484 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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