Meloxicam (Mobic)
(Synonyms: 美洛昔康) 目录号 : GC11762
A selective COX-2 inhibitor
Cas No.:71125-38-7
Sample solution is provided at 25 µL, 10mM.
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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.
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].
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].
Reference：
[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 experiment: | 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]. |
Animal experiment: | 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]. |
References: [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. | |
| Cas No. | 71125-38-7 | SDF | |
| 别名 | 美洛昔康 | ||
| 化学名 | 4-hydroxy-2-methyl-N-(5-methyl-1,3-thiazol-2-yl)-1,1-dioxo-1λ6,2-benzothiazine-3-carboxamide | ||
| Canonical SMILES | CC1=CN=C(S1)NC(=O)C2=C(C3=CC=CC=C3S(=O)(=O)N2C)O | ||
| 分子式 | C14H13N3O4S2 | 分子量 | 351.4 |
| 溶解度 | ≥ 17.57mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50%
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