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Mavacoxib (PHA-739521)

This product is for research use only, not for human use. We do not sell to patients.

Mavacoxib (PHA-739521)
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Cat #: V25071 CAS #: 170569-88-7 Purity ≥ 99%

Description: Mavacoxib (PHA-739521), a long-acting non-steroidal anti-inflammatory drug (NSAID), is a selective, orally active and long-acting cyclooxygenase-2 (COX-2) inhibitor used to treat pain and inflammation associated with degenerative joint disease in dogs.

References: Hurst EA, et al. The selective cyclooxygenase-2 inhibitor mavacoxib (Trocoxil) exerts anti-tumour effects in vitro independent of cyclooxygenase-2 expression levels. Vet Comp Oncol. 2019 Jun;17(2):194-207.

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Molecular Weight (MW)385.34
Molecular FormulaC16H11F4N3O2S
CAS No.170569-88-7
SMILES CodeO=S(C1=CC=C(N2N=C(C(F)(F)F)C=C2C3=CC=C(F)C=C3)C=C1)(N)=O
SynonymsPHA-739521; PHA739521; PHA 739521; PHA 739,521; PHA739,521; PHA-739,521; Mavacoxib. trade name Trocoxil.
ProtocolIn VitroMavacoxib (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. 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. 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.
In VivoOsteoarthritic 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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.5951 mL12.9756 mL25.9511 mL51.9022 mL
5mM0.5190 mL2.5951 mL5.1902 mL10.3804 mL
10mM0.2595 mL1.2976 mL2.5951 mL5.1902 mL
20mM0.1298 mL0.6488 mL1.2976 mL2.5951 mL
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%DMSO + % + %Tween 80 + %ddH2O

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Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
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