Meloxicam(Synonyms: 美洛昔康)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Meloxicam (Synonyms: 美洛昔康) 纯度: 99.88%

Meloxicam 是一种非甾体类抗炎剂,能够有效抑制 COX 的活性,对 COX-2 和 COX-1 的 IC50 值分别为 0.49 µM 和 36.6 µM。

Meloxicam(Synonyms: 美洛昔康)

Meloxicam Chemical Structure

CAS No. : 71125-38-7

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生物活性

Meloxicam is a non-steroidal antiinflammatory agent, inhibits COX activity, with IC50s of 0.49 µM and 36.6 µM for COX-2 and COX-1, respectively.

IC50 & Target[1]

COX-2

0.49 μM (IC50)

COX-1

36.6 μM (IC50)

体外研究
(In Vitro)

Meloxicam (Compound 5) is a non-steroidal antiinflammatory agent, inhibits COX activity, with IC50s of 0.49 µM and 36.6 µM for COX-2 and COX-1, respectively[1]. Meloxicam inhibits COX+ tumor cells, but shows no cytotoxicity on CF41.Mg or MDCK cells at 0.25-25 µg/mL. Furthermore, Meloxicam in combination with doxorubicin, has no synergistic effect on CF41.Mg cells. Meloxicam (0.25 µg/mL) decreases CF41.Mg cell migration and invasion, induces decrease in MMP-2 expression, and increases β-catenin phophorylation in CF41.Mg cells, but does not affect the CF41.Mg cell apoptosis[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Meloxicam (10 mg/kg) alone or in combination with rutin significantly decreases paw liking time on 1st day by 55% and 49% compared with the formalin-treated group, respectively, however the combination reduces time non-significantly on 3rd day in mice. Meloxicam alone or in combination with rutin also decreases relative liver weights, reduces MDA contents, induces liver SOD activities, hampers IL-1β content, and significantly reduces the number of positive caspase-3 immunoreactive cells in mice[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

351.40

Formula

C14H13N3O4S2

CAS 号

71125-38-7

中文名称

美洛昔康

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (142.29 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8458 mL 14.2288 mL 28.4576 mL
5 mM 0.5692 mL 2.8458 mL 5.6915 mL
10 mM 0.2846 mL 1.4229 mL 2.8458 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,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,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.11 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.11 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1 mg/mL (2.85 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (2.85 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 10.0 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 ddH₂O 中,得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Lazer ES, et al. Effect of structural modification of enol-carboxamide-type nonsteroidal antiinflammatory drugs on COX-2/COX-1 selectivity. J Med Chem. 1997 Mar 14;40(6):980-9.

    [2]. Iturriaga MP, et al. Meloxicam decreases the migration and invasion of CF41.Mg canine mammary carcinoma cells. Oncol Lett. 2017 Aug;14(2):2198-2206.

    [3]. Fikry EM, et al. Rutin and meloxicam attenuate paw inflammation in mice: Affecting sorbitol dehydrogenase activity. J Biochem Mol Toxicol. 2018 Feb;32(2).

Cell Assay
[2]

CF41.Mg and MDCK cells are seeded at a density of 1.5 × 103 cells/well into 96-well plates, cultured for 24 h and then exposed to 0-25 µg/mL Meloxicam alone or in combination with doxorubicin. To evaluate synergism and sensitization, doxorubicin is added at the same time and after 24 h, respectively. MDCK cells are exposed only to Meloxicam as a non-tumor negative control. Control groups are cultured without Meloxicam and doxorubicin, but the corresponding amount of DMSO is added to the medium. Following an incubation period of 24 and 48 h, cell growth is measured using the MTS assay, with the absorbance at 490 nm determined using a microplate reader. Each experiment is performed 3 times in triplicate[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Mice[3]
Thirty-two mice are randomLy allocated into four groups, eight mice each. Groups are received 20 μL of 2.5% formalin injected in the plantar region of the right hind paw of mice on the 1st and 3rd days 1 h after administration of 1% DMSO (group 1; positive control group), 60 mg/kg rutin, orally (group 2), and oral treatment with 10 mg/kg Meloxicam (group 3), as well as combined treatment of rutin and Meloxicam (group 4). In all groups, drugs are administered once a day for duration of 7 days. On day 7, mice are euthanized and right hind paws plus livers are immediately excised, washed with ice-cold saline, blotted dry, and weighed. They are stored at −80°C till the time of analysis. Then the used animals will be frozen till being incinerated[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Lazer ES, et al. Effect of structural modification of enol-carboxamide-type nonsteroidal antiinflammatory drugs on COX-2/COX-1 selectivity. J Med Chem. 1997 Mar 14;40(6):980-9.

    [2]. Iturriaga MP, et al. Meloxicam decreases the migration and invasion of CF41.Mg canine mammary carcinoma cells. Oncol Lett. 2017 Aug;14(2):2198-2206.

    [3]. Fikry EM, et al. Rutin and meloxicam attenuate paw inflammation in mice: Affecting sorbitol dehydrogenase activity. J Biochem Mol Toxicol. 2018 Feb;32(2).

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