Nimesulide D5
(Synonyms: 尼美舒利 D5) 目录号 : GC39583
An internal standard for the quantification of nimesulide
Cas No.:1330180-22-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Nimesulide-d5 is intended for use as an internal standard for the quantification of nimesulide by GC- or LC-MS. Nimesulide is a non-steroidal anti-inflammatory drug (NSAID) and COX-2 inhibitor (IC50s = 1.27 and 0.03 ?M for the human and ovine enzymes, respectively).1,2 It is selective for COX-2 over COX-1 (IC50s = 70 and 22 ?M for the human and ovine enzymes, respectively). Nimesulide also inhibits sodium-dependent neutral amino acid transporter (B0AT1) with an IC50 value of 23 ?M for the rat kidney transporter.3 It inhibits infection-induced increases in brain prostaglandin E2 levels, as well as reduces pyresis (ED50 = 0.3 mg/kg), in yeast-infected rats.4 Nimesulide (2.9 mg/kg) inhibits formalin-induced hindpaw thermal hyperalgesia in rats.5
1.Johnson, J.L., Wimsatt, J., Buckel, S.D., et al.Purification and characterization of prostaglandin H synthase-2 from sheep placental cotyledonsArch. Biochem. Biophys.324(1)26-34(1995) 2.Barnett, J., Chow, J., Ives, D., et al.Purification, characterization and selective inhibition of human prostaglandin G/H synthase 1 and 2 expressed in the baculovirus systemBiochim. Biophys. Acta1209(1)130-139(1994) 3.Pochini, L., Seidita, A., Sensi, C., et al.Nimesulide binding site in the B0AT1 (SLC6A19) amino acid transporter. Mechanism of inhibition revealed by proteoliposome transport assay and molecular modellingBiochem. Pharmacol.89(3)422-430(2014) 4.Taniguchi, Y., Yokoyama, K., Inui, K., et al.Inhibition of brain cyclooxygenase-2 activity and the antipyretic action of nimesulideEur. J. Pharmacol.330221-229(1997) 5.Bianchi, M., and Broggini, M.Anti-hyperalgesic effects of nimesulide: Studies in rats and humansInt. J. Clin. Pract. Suppl.57(128)11-19(2002)
| Cas No. | 1330180-22-7 | SDF | |
| 别名 | 尼美舒利 D5 | ||
| Canonical SMILES | CS(=O)(NC1=CC=C([N+]([O-])=O)C=C1OC2=C([2H])C([2H])=C([2H])C([2H])=C2[2H])=O | ||
| 分子式 | C13H7D5N2O5S | 分子量 | 313.34 |
| 溶解度 | Methanol: soluble | 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 | 3.1914 mL | 15.9571 mL | 31.9142 mL |
| 5 mM | 0.6383 mL | 3.1914 mL | 6.3828 mL |
| 10 mM | 0.3191 mL | 1.5957 mL | 3.1914 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。
Simultaneous determination of nimesulide and its four possible metabolites in human plasma by LC-MS/MS and its application in a study of pharmacokinetics
J Chromatogr B Analyt Technol Biomed Life Sci 2016 Aug 1;1027:139-48.PMID:27284972DOI:10.1016/j.jchromb.2016.05.008.
In this study, it was the first time that we simultaneously quantified nimesulide and its possible metabolites M1, M2, M3 and M4 by employing liquid chromatography-tandem mass spectrometry (LC-MS/MS). Nimesulide-D5 was used as internal standard (IS) for validation. Analytes and IS were recovered from human plasma by protein precipitation with acetonitrile. Prepared plasma samples were analyzed under the same LC-MS/MS conditions, and chromatographic separation was realized by using an Ultimate C18 column, with run time being 5min for each sample. Our results showed that various analytes within their concentration ranges could be quantified accurately by using the method. Mean intra- and inter-day accuracies ranged from -4.8% to 4.8% (RE), and intra- and inter-assay precision ≤6.2% (RSD). The following parameters were validated: specificity, recovery, matrix effects, dilution integrity, carry-over, sample stability under a variety of storage and handling conditions (room temperature, freezer, freeze-thaw and post-preparative) and stock solution stability. Pharmacokinetics of nimesulide and its metabolites were calculated based on the analysis of samples collected from twelve Chinese healthy volunteers after single oral dose of 100mg nimesulide tablets. By applying the pharmacokinetic determination into human samples, we preliminarily detected a new metabolite of nimesulide (M4*), and the concentration of M4* was relatively higher in plasma. Furthermore, we predicted part of conceivable metabolism pathway in plasma of after oral administration of 100mg nimesulide tablets. This research provided an experimental basis for further studies on metabolic activation and biotransformation of nimesulide, and for more comprehensive conjecture of its metabolic pathways.