Valdecoxib

- Overview
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    Background
    
    Valdecoxib is a potent and selective inhibitor of cyclooxygenase-2 (COX-2) with IC50 value of 5nM [1].
    Valdecoxib is developed for the management 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. Moreover, oral administration of valdecoxib exerts chronic anti-inflammatory activity with ED50 value of 0.032 mg/kg/day in the rat adjuvant arthritis model. In addition, valdecoxib is reported to have cardiovascular risk adverse effect in patients undergoing CABG [1, 2].
    
    [1] Talley J J, Brown D L, Carter J S, et al. 4-[5-Methyl-3-phenylisoxazol-4-yl]-benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2. Journal of medicinal chemistry, 2000, 43(5): 775-777.
    [2] Nussmeier N A, Whelton A A, Brown M T, et al. Complications of the COX-2 inhibitors parecoxib and valdecoxib after cardiac surgery. New England Journal of Medicine, 2005, 352(11): 1081-1091.
- Properties
  - Alternative Name
    
    4-(5-methyl-3-phenyl-1,2-oxazol-4-yl)benzenesulfonamide
    
    CAS Number
    
    181695-72-7
    
    Molecular Formula
    
    C16H14N2O3S
    
    Molecular Weight
    
    314.36
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥15.72 mg/mL in DMSO; ≥5.42 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Valdecoxib

Background

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