Mavacoxib.|170569-88-7|-陌孚医药/Medlife

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Mavacoxib.

目录号: PC22004 纯度: 98%

CAS No. :170569-88-7

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中文名称

Mavacoxib.

中文别名

吗伐考昔;1-(三甲基硅基)哌啶;3''-氯联苯-3-羧酸;3-氯联苯-3-羧酸;4-[5-(4-氟苯基)-3-(三氟甲基)吡唑-1-基]苯磺酰胺

英文名称

4-[5-(4-FLUOROPHENYL)-3-(TRIFLUOROMETHYL)PYRAZOL-1-YL]BENZENE-1-SULFONAMIDE

英文别名

4-[5-(4-FLUOROPHENYL)-3-(TRIFLUOROMETHYL)PYRAZOL-1-YL]BENZENE-1-SULFONAMIDE;4-[5-(4-fluorophenyl)-3-(trifluoromethyl)pyrazol-1-yl]benzenesulfonamide;Mavacoxib;PHA 739,521;4-[5-(4-Fluorophenyl)-3-trifluoromethyl-1H-pyrazol-1-yl]benzenesulfonamide;PHA 739521;Trocoxil;4-[5-(4-Fluoro-phenyl)-3-trifluoromethyl-pyrazol-1-yl]-benzenesulfonamide;4-[5-(4-Fluorophenyl)-3-trifluoroMethyl-1H-pyrazol-1-yl] benzenesulfonaMide;BenzenesulfonaMide, 4-[5-(4-fluorophenyl)-3-(trifluoroMethyl)-1H-pyrazol-1-yl]-

Cas No.

170569-88-7

分子式

C₁₆H₁₁F₄N₃O₂S

分子量

385.34

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

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.

性状

Solid

IC50 & Target[1][2]

COX-2

体外研究(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.
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 (0-75 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.

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

Cell Viability Assay

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

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

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.

体内研究(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.

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

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Hurst EA, et al. The selective cyclooxygenase-2 inhibitor mavacoxib (Trocoxil) exerts anti-tumour effects 体外研究 independent of cyclooxygenase-2 expression levels. Vet Comp Oncol. 2019 Jun;17(2):194-207. [Information]

[2]. Cox SR, et al. Population pharmacokinetics of mavacoxib in osteoarthritic dogs. J Vet Pharmacol Ther. 2011 Feb;34(1):1-11. [Information]

溶解度数据

体外研究:

DMSO : 250 mg/mL (648.78 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	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
10 mM	0.2595 mL	1.2976 mL	2.5951 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.40 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.40 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.40 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.40 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.40 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.40 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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