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CAS No.: 170569-88-7

Mavacoxib/吗伐考昔 Catalog No. CSN20674

Synonyms: Trocoxil;PHA-739512;PHA-739521

Mavacoxib is a veterinary drug used to treat pain and inflammation in dogs with degenerative joint disease. It acts as a COX-2 inhibitor.

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技术信息

生物活性

描述The inflammatory enzyme cyclooxygenase-2 (COX-2) is a tumor promoter that can be stimulated by inflammatory cytokines and growth factors. Mavacoxib is a COX-2 inhibitor that reduces the viability of a panel of canine and human cancer cell lines (i.e. U2OS, KTOSA5, CSKOS, REM, LILY, K9TCC, K9TCC-AXA, K9TCC-In, K9TCC-Sh, T24, 5637, HT-1376) in a concentration-dependent manner with IC50 values ranging from 34.5–157.7μM. Mavacoxib at concentrations of 25–75μM induced replicative cell death in tested cancer cell lines. Mavacoxib treatment also inhibited the migration of KTOSA5, U2OS, REM, LILY, K9TCC, and T24 cells at 50, 50, 50, 100, 75, and 125μM^[3]. Mavacoxib exhibited broad between-subject variability and apparent volume of distribution in dogs with coefficients of variation of 47% and 19%, respectively. The typical terminal elimination plasma half-life of mavacoxib was 44 days. Osteoarthritic dogs treated with mavacoxib at 2mg/kg maintained plasma mavacoxib concentration associated with efficacy^[4].
参考文献

[1] Dhondt L, Devreese M, et al. Comparative population pharmacokinetics and absolute oral bioavailability of COX-2 selective inhibitors celecoxib, mavacoxib and meloxicam in cockatiels (Nymphicus hollandicus). Sci Rep. 2017 Sep 25;7(1):12043.
[2] Pang LY, Argyle SA, et al. The long-acting COX-2 inhibitor mavacoxib (Trocoxil™) has anti-proliferative and pro-apoptotic effects on canine cancer cell lines and cancer stem cells in vitro. BMC Vet Res. 2014 Sep 5;10:184.
[3] Hurst EA, Pang LY, Argyle DJ. 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.
[4] Cox SR, Liao S, Payne-Johnson M, Zielinski RJ, Stegemann MR. Population pharmacokinetics of mavacoxib in osteoarthritic dogs. J Vet Pharmacol Ther. 2011 Feb;34(1):1-11.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5951 mL
- 12.9757 mL
- 25.9514 mL
- 5 mM
- 0.5190 mL
- 2.5951 mL
- 5.1903 mL
- 10 mM
- 0.2595 mL
- 1.2976 mL
- 2.5951 mL

技术信息

CAS号

170569-88-7

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H11F4N3O2S

运输

蓝冰

分子量

385.34

别名

Trocoxil;PHA-739512;PHA-739521;PHA-739,521

溶解度

DMSO	77.0 mg/mL (199.8 mM)
Water	Insoluble
Ethanol	75.0 mg/mL (194.6 mM)

动物实验配方

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Mavacoxib/吗伐考昔 Catalog No. CSN20674

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