Valdecoxib

Catalog No.S4049

Valdecoxib Chemical Structure

Molecular Weight(MW): 314.36

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

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In DMSO USD 140 In stock
USD 110 In stock
USD 470 In stock
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1 Customer Review

  • (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.
Targets
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]

Protocol

Animal Research:[1]
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  • Animal Models: Male Sprague-Dawley rats
  • Formulation: 0.5% methyl cellulose and 0.025% Tween-20
  • 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 individually and in order:
0.5% methylcellulose+0.2% Tween 80
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
Formula

C16H14N2O3S

CAS No. 181695-72-7
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00260325 Completed Pain|Hyperalgesia Penn State University|Pfizer|National Institutes of Health (NIH) August 2004 Phase 4
NCT00660855 Terminated Pain, Post Surgical Pfizer June 2004 Phase 4
NCT00652808 Completed Osteoarthritis|Knee Pfizer May 2004 Phase 3
NCT00650039 Completed Pain Pfizer March 2004 Phase 3
NCT00650598 Completed Pain, Postoperative Pfizer March 2004 Phase 4
NCT01541137 Completed Postoperative Pain Helsinki University Central Hospital|Academy of Finland March 2004 --

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COX Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID