2. Immunology/Inflammation
  3. COX
  4. Mavacoxib

Mavacoxib is a selective, oral long-acting cyclooxygenase-2 (COX-2) inhibitor and a long-acting non-steroidal anti-inflammatory drug (NSAID). Mavacoxib is used to treat pain and inflammation associated with degenerative joint disease in dogs.

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Mavacoxib Chemical Structure

Mavacoxib Chemical Structure

CAS No. : 170569-88-7

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Based on 1 publication(s) in Google Scholar

Other Forms of Mavacoxib:

Mavacoxib Related Antibodies

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  • Biological Activity

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Description

Mavacoxib is a selective, oral long-acting cyclooxygenase-2 (COX-2) inhibitor and a long-acting non-steroidal anti-inflammatory drug (NSAID). Mavacoxib is used to treat pain and inflammation associated with degenerative joint disease in dogs[1].

IC50 & Target[1]

COX-2

 

In Vitro

Mavacoxib (0-200 μM; 72 hours; CSKOS, U2OS, REM, K9TCC and T24 cells) treatment reduces cell viability in a dose-dependent manner. However, sensitivity to Mavacoxib varied between the cell lines, with IC50 values ranging from 34.5 μM to 157.7 μM. The IC50 values of U2OS, KTOSA5, CSKOS, REM, LILY, K9TCC, K9TCC-AXA, K9TCC-In, K9TCC-Sh, T24, 5637 and HT-1376 cells are 52.6 μM, 89.8 μM, 106.3 μM, 66.6 μM, 97.5 μM, 54.9 μM, 34.5 μM, 78.7 μM, 50.7 μM, 63.4 μM, 72.5 μM and 157.7 μM, respectively[1].
Mavacoxib (0-200 μM; 48 hours; KTOSA5, REM, LILY, K9TCC, U2OS, and T24 cells) treatment can induce caspase-dependent apoptosis in a number of cell lines[1].
Mavacoxib (0-75 μM; 24 hours; CSKOS, U2OS, REM, K9TCC and T24 cells) treatment down-regulates the expression of p-Akt in CSKOS cells in in a dose-dependent manner, as is total Akt in U2OS cells. In REM cells, both p-ERK and p-Akt are increased in expression with increasing doses of Mavacoxib, and in K9TCC cells p-ERK expression is also increased with Mavacoxib treatment[1].

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

Mavacoxib Related Antibodies

Cell Viability Assay[1]

Cell Line: CSKOS, U2OS, REM, K9TCC and T24 cells
Concentration: 0 μM, 0.04 μM, 25 μM, 50 μM, 75 μM, 100 μM, 125 μM, 150 μM, 175 μM, 200 μM
Incubation Time: 72 hours
Result: Cell viability was reduced in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: KTOSA5, REM, LILY, K9TCC, U2OS, and T24 cells
Concentration: 0 μM, 50 μM, 100 μM, 200 μM
Incubation Time: 48 hours
Result: Induced apoptosis in canine and human cancer cell lines.

Cell Viability Assay[1]

Cell Line: CSKOS, U2OS, REM, K9TCC and T24 cells
Concentration: 0 μM, 25 μM, 50 μM or 75 μM
Incubation Time: 24 hours
Result: In CSKOS cells, p-Akt was downregulated, as was total Akt in U2OS cells. In REM cells, both p-ERK and p-Akt were increased in expression, and in K9TCC cells p-ERK expression was also increased.
In Vivo

Osteoarthritic dogs enrolled in the studies are randomized to receive treatment with Mavacoxib and daily placebo for carprofen or placebo for Mavacoxib and daily carprofen at a nominal dose of 4 mg/kg BW. Mavacoxib is administered in both studies with a 2-week interval between the first and second doses but with monthly dosing thereafter. The nominal Mavacoxib doses in Studies 1 and 2 are 4 and 2 mg/kg BW, respectively. Seven Mavacoxib doses are administered in Study 1, but only five doses in Study 2. In Study 1, Mavacoxib is administered without regard to the timing of meals, but in Study 2, all of the Mavacoxib doses are administered with food[2].

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

385.34

Formula

C16H11F4N3O2S
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=S(C1=CC=C(N2N=C(C(F)(F)F)C=C2C3=CC=C(F)C=C3)C=C1)(N)=O
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 : 100 mg/mL (259.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5951 mL 12.9756 mL 25.9511 mL
5 mM 0.5190 mL 2.5951 mL 5.1902 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
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Concentration
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Volume
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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: ≥ 2.08 mg/mL (5.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 99.04%

SDS (419 KB)

COA (254 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
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 2.5951 mL 12.9756 mL 25.9511 mL 64.8778 mL
5 mM 0.5190 mL 2.5951 mL 5.1902 mL 12.9756 mL
10 mM 0.2595 mL 1.2976 mL 2.5951 mL 6.4878 mL
15 mM 0.1730 mL 0.8650 mL 1.7301 mL 4.3252 mL
20 mM 0.1298 mL 0.6488 mL 1.2976 mL 3.2439 mL
25 mM 0.1038 mL 0.5190 mL 1.0380 mL 2.5951 mL
30 mM 0.0865 mL 0.4325 mL 0.8650 mL 2.1626 mL
40 mM 0.0649 mL 0.3244 mL 0.6488 mL 1.6219 mL
50 mM 0.0519 mL 0.2595 mL 0.5190 mL 1.2976 mL
60 mM 0.0433 mL 0.2163 mL 0.4325 mL 1.0813 mL
80 mM 0.0324 mL 0.1622 mL 0.3244 mL 0.8110 mL
100 mM 0.0260 mL 0.1298 mL 0.2595 mL 0.6488 mL
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Mavacoxib Related Classifications

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.

Keywords:

Mavacoxib170569-88-7COXCyclooxygenaseInhibitorinhibitorinhibit

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