1. Immunology/Inflammation Metabolic Enzyme/Protease
  2. COX Endogenous Metabolite
  3. Valdecoxib

Valdecoxib  (Synonyms: SC 65872)

Cat. No.: HY-15762 Purity: 99.96%
COA Handling Instructions

Valdecoxib is a highly potent and selective inhibitor of COX-2, with IC50s of 5 nM and 140 μM for COX-2 and COX-1, respeceively. Valdecoxib can be used in the research of arthritis and pain.

For research use only. We do not sell to patients.

Valdecoxib Chemical Structure

Valdecoxib Chemical Structure

CAS No. : 181695-72-7

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Solid + Solvent
10 mM * 1 mL in DMSO
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USD 129 In-stock
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10 mM * 1 mL in DMSO USD 129 In-stock
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10 mg USD 117 In-stock
50 mg USD 488 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Valdecoxib:

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Valdecoxib is a highly potent and selective inhibitor of COX-2, with IC50s of 5 nM and 140 μM for COX-2 and COX-1, respeceively. Valdecoxib can be used in the research of arthritis and pain.

IC50 & Target[1]

COX-2

5 nM (IC50)

COX-1

140 μM (IC50)

Human Endogenous Metabolite

 

In Vitro

Valdecoxib (Compound 2) is a highly potent, selective and orally active inhibitor of COX-2, with IC50s of 5 nM and 140 μM for COX-2 and COX-1, respeceively[1]. Valdecoxib (10, 100 µM) inhibits LPS-induced proliferation of endothelial cells and bFGF secretion in a dose-dependent manner. Valdecoxib stimulates VEGF formation via HMEC-1 under inflammatory conditions[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Valdecoxib (Compound 2) shows potent oral activity in an acute antiinflammatory assay (rat carrageenan foot pad edema; ED50 = 10.2 ± 1.4 mg/kg). Valdecoxib also has chronic antiinflammatory activity in the rat adjuvant arthritis model, with an ED50 of 0.032 ± 0.002 mg/kg/day[1]. Valdecoxib (10 mg/kg, i.p.) significantly attenuates the behavioral and biochemical (oxidative damage) alterations in chronic-stressed mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

314.36

Formula

C16H14N2O3S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC=C(C2=C(C)ON=C2C3=CC=CC=C3)C=C1)(N)=O

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 34 mg/mL (108.16 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1811 mL 15.9053 mL 31.8107 mL
5 mM 0.6362 mL 3.1811 mL 6.3621 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.96%

References
Cell Assay
[2]

HMEC-1 cells proliferation is measured using the MTT conversion method. Cells are seeded (50.000 cells/well) into 96-well plates. The cells are incubated for 24 h with LPS 100 µg/mL, CoCl2 200 µM, Valdecoxib 10 or 100 µM, LPS and Valdecoxib or CoCl2 and Valdecoxib or without tested chemicals (control group). All the substances are added at the same time. After incubation, 50 µL MTT (1 mg/mL) is added and the plates are incubated at 37°C for 4 h. At the end of the experiment, cells are exposed to 100 µL DMSO, which enables the release of the blue reaction product-formazan. The absorbance at 570 nm is read on a microplate reader and results are expressed as a percentage of the absorbance measured in control cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Mice[3]
The drugs including naproxen (14 mg/kg, i.p.), rofecoxib (5 mg/kg, i.p.), meloxicam (5 mg/kg, i.p.), nimesulide (5 mg/kg, i.p.) and Valdecoxib (10 mg/kg, i.p.) are used in the assay. The animals are randomized into 7 groups (n=10 in each group), including the naive group, in which the mice only receive vehicle for 15 d without forced swimming session; the control (chronically stressed) group, in which mice receive vehicle 30 min before the forced swimming session (6 min) for 15 d; the naproxen (14 mg/kg) group; the Valdecoxib (10 mg/kg) group; the rofecoxib (5 mg/kg) group; the meloxicam (5 mg/kg) group; and the nimesulide (5 mg/kg) group. Drugs are suspended in 0.25% carboxymethylcellulose (CMC) and administered intraperitoneally, 30 min before the forced swimming session for 15 consecutive days[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1811 mL 15.9053 mL 31.8107 mL 79.5267 mL
5 mM 0.6362 mL 3.1811 mL 6.3621 mL 15.9053 mL
10 mM 0.3181 mL 1.5905 mL 3.1811 mL 7.9527 mL
15 mM 0.2121 mL 1.0604 mL 2.1207 mL 5.3018 mL
20 mM 0.1591 mL 0.7953 mL 1.5905 mL 3.9763 mL
25 mM 0.1272 mL 0.6362 mL 1.2724 mL 3.1811 mL
30 mM 0.1060 mL 0.5302 mL 1.0604 mL 2.6509 mL
40 mM 0.0795 mL 0.3976 mL 0.7953 mL 1.9882 mL
50 mM 0.0636 mL 0.3181 mL 0.6362 mL 1.5905 mL
60 mM 0.0530 mL 0.2651 mL 0.5302 mL 1.3254 mL
80 mM 0.0398 mL 0.1988 mL 0.3976 mL 0.9941 mL
100 mM 0.0318 mL 0.1591 mL 0.3181 mL 0.7953 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Valdecoxib
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