美洛昔康作用机制 - Medchemexpress - MCE中国

1、Product Data SheetMeloxicamCat. No.: HY-B0261CAS No.: 71125-38-7分式: CHNOS分量: 351.4作靶点: COX; Autophagy; Apoptosis作通路: Immunology/Inflammation; Autophagy; Apoptosis储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (142.29 mM; Need ultrasonic)H2O : 0.1 mg/m

2、L (insoluble)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 2.8458 mL 14.2288 mL 28.4576 mL5 mM 0.5692 mL 2.8458 mL 5.6915 mL10 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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据

3、您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 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 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.11 mM); Suspended solution; Need ultrasonic此案可获得 2

4、.5 mg/mL (7.11 mM) 的均匀悬浊液，悬浊液可于服和腹腔注射。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.11 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.5 mg/mL (7.11 mM，饱和度未知) 的澄 溶液，此案不适于

5、实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Meloxicam 36.6 M。种甾体类抗炎剂，能够有效抑制 COX 的活性，对 COX-2 和 COX-1 的 IC50 值分别为 0.49 M 和IC & Target COX-2 COX-10.49 M (IC50) 36.6 M (IC50)体外研究 Meloxicam (Compound 5) is a non-steroidal antiinflammatory agent, inhibit

6、s COX activity, with IC50s of 0.49 M and36.6 M for COX-2 and COX-1, respectively1. Meloxicam inhibits COX+ tumor cells, but shows no cytotoxicity onCF41.Mg or MDCK cells at 0.25-25 g/mL. Furthermore, Meloxicam in combination with doxorubicin, has nosynergistic effect on CF41.Mg cells. Meloxicam (0.2

7、5 g/mL) decreases CF41.Mg cell migration and invasion, inducesdecrease in MMP-2 expression, and increases -catenin phophorylation in CF41.Mg cells, but does not affect theCF41.Mg cell apoptosis2.体内研究 Meloxicam (10 mg/kg) alone or in combination with rutin significantly decreases paw liking time on 1

8、st 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-1

9、content, and significantly reduces the number ofpositive caspase-3 immunoreactive cells in mice3.PROTOCOLCell 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 andthen exposed to 0-25 g/mL Meloxicam alone or in combination with doxoru

10、bicin. To evaluate synergism andsensitization, doxorubicin is added at the same time and after 24 h, respectively. MDCK cells are exposed only toMeloxicam as a non-tumor negative control. Control groups are cultured without Meloxicam and doxorubicin, butthe corresponding amount of DMSO is added to t

11、he medium. Following an incubation period of 24 and 48 h, cellgrowth is measured using the MTS assay, with the absorbance at 490 nm determined using a microplate reader. Eachexperiment is performed 3 times in triplicate2.MCE has not independently confirmed the accuracy of these methods. They are for

12、 reference only.Animal Mice3Administration 3 Thirty-two mice are randomLy allocated into four groups, eight mice each. Groups are received 20 L 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 administrationof 1% DMSO (group 1; positive c

13、ontrol group), 60 mg/kg rutin, orally (group 2), and oral treatment with 10 mg/kgMeloxicam (group 3), as well as combined treatment of rutin and Meloxicam (group 4). In all groups, drugs areadministered once a day for duration of 7 days. On day 7, mice are euthanized and right hind paws plus livers

14、areimmediately excised, washed with ice-cold saline, blotted dry, and weighed. They are stored at 80C till the time ofanalysis. Then the used animals will be frozen till being incinerated3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCESPage 2

15、 of 3 www.MedChemE1. 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. 2