For research use only.
CAS No. 181695-72-7
Valdecoxib is a potent and selective inhibitor of COX-2 with IC50 of 5 nM.
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Choose Selective COX Inhibitors
|Description||Valdecoxib is a potent and selective inhibitor of COX-2 with IC50 of 5 nM.|
|Features||Valdecoxib is more potent in inhibiting COX-2 than COX-1.|
Valdecoxib inhibits LPS-induced PGE2 production in plasma with IC50 of 0.89 μM for assessment of the extent of COX-2 inhibition. Valdecoxib inhibits TxB2 production in plasma with IC50 of 25.4 μM for assessment of the extent of COX-1 inhibition.  Valdecoxib binds to COX-2 with Ka of 1.1×105 M/s. The overall saturation binding affinity for COX-2 of Valdecoxib is 2.6 nM. Valdecoxib shows similar activity in the human whole-blood COX assay (COX-2 IC50 = 0.24 μM; COX-1 IC50 = 21.9 μM).  The affinity of [3H]Valdecoxib for COX-2 with KD of 3.2 nM. The binding of Valdecoxib to COX-2 seems to be both rapid and slowly reversible with association rates of 4.5 × 106/M/min and dissociation rates of 7.0 × 10-3/min (t1/2 of 98 min).  The percent of dissolved Valdecoxib at 15 min (DP15) is 10.5% for Valdecoxib and 50%, 91% and 93% for its hydrophilic derivatives (VALD-βCd, VALD-HPβCd and VALD-SBE7βCd complexes), respectively. 
|In vivo||Valdecoxib administrated orally inhibits rat carrageenan foot pad edema with ED50 of 10.2 mg/kg. Valdecoxib administrated orally shows chronic antiinflammatory activity with ED50 of 0.032 mg/kg/day in rat adjuvant arthritis model. Valdecoxib administrated orally shows blockade of prostaglandin production at the inflammatory site with ED50 of 0.02 mg/kg in the rat carrageenan air pouch model.  Valdecoxib demonstrates marked potency in acute and chronic models of inflammation (air pouch ED50 = 0.06 mg/kg; paw edema ED50 = 5.9 mg/kg; adjuvant arthritis ED50 = 0.03 mg/kg) in rats.  Valdecoxib alone shows slow in vivo absorption giving maximum % inhibition of edema (16%) after a period of 3 hour. In contrast, VALD-βCd and VALD-SBE7βCd complexes shows high absorption rate in vivo achieving more than 50% inhibition of edema in the 1 hour and maximum percentage of inhibition of edema (66%) after a period of 3 hours.  Valdecoxib (5 mg/kg, po) results in AUC in plasma of 3.58 μg*h/mL and 2.08 μg*h/mL in males and female mice, respectively. Valdecoxib (5 mg/kg, po) results in AUC red blood cells of 12.1 μg*h/mL and 6.42 μg*h/mL in males and female mice, respectively. |
-  Talley JJ, et al. J Med Chem, 2000, 43(5), 775-777.
-  Gierse JK, et al. J Pharmacol Exp Ther, 2005, 312(3), 1206-12012.
-  Hood WF, et al. Mol Pharmacol, 2003, 63(4), 870-877.
|In vitro||DMSO||63 mg/mL (200.4 mM)|
|Ethanol||18 mg/mL (57.25 mM)|
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0.5% methylcellulose+0.2% Tween 80
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00122096||Completed||Drug: valdecoxib||Neurosurgery|Pain||University of Washington|Pfizer||November 2002||Phase 4|
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