For research use only.

Catalog No.S4049

1 publication

Valdecoxib Chemical Structure

Molecular Weight(MW): 314.36

Valdecoxib is a potent and selective inhibitor of COX-2 with IC50 of 5 nM.

Size Price Stock Quantity  
10mM (1mL in DMSO) RMB 1151.44 In stock
RMB 902.13 In stock
RMB 3845.72 In stock
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Selleck's Valdecoxib has been cited by 1 publication

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  • (B) HeLa and SACC-83 cells were treated with radiation, valdecoxib, or both radiation and valdecoxib. Cells were lysed or extracted for membrane proteins and then subjected to Western blot.

    Biochem Biophys Res Commun, 2015, 460(2):198-204. . Valdecoxib purchased from Selleck.

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Biological Activity

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.
COX-2 [1]
5 nM
In vitro

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. [1] 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). [2] 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). [3] 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. [4]

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. [1] 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. [2] 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. [4] 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. [5]


Animal Research:[1]
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  • Animal Models: Male Sprague-Dawley rats
  • Dosages: 10.2 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 63 mg/mL (200.4 mM)
Ethanol 18 mg/mL (57.25 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% methylcellulose+0.2% Tween 80
For best results, use promptly after mixing.
19 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 314.36


CAS No. 181695-72-7
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C(C(=NO1)C2=CC=CC=C2)C3=CC=C(C=C3)S(=O)(=O)N

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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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COX Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID