4-hydroxy Diclofenac
(Synonyms: 4′-羟基双氯芬酸) 目录号 : GC42407A CYP2C9 metabolite of the NSAID diclofenac
Cas No.:64118-84-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >97.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
4-hydroxy Diclofenac is a CYP2C9 metabolite of the NSAID diclofenac.[1] [2] [3] By inhibiting COX and subsequently suppressing PGE2 synthesis, it demonstrates anti-inflammatory and analgesic properties.[4]
Reference:
[1]. Shimamoto, J., Ieiri, I., Urae, A., et al. Lack of differences in diclofenac (a substrate for CYP2C9) pharmacokinetics in healthy volunteers with respect to the single CYP2C9*3 allele. European Journal of Clinical Pharmacology 56, 65-68 (2000).
[2]. Sawchuk, R.J., Maloney, J.A., Cartier, L.L., et al. Analysis of diclofenac and four of its metabolites in human urine by HPLC. Pharm. Res. 12(5), 756-762 (1995).
[3]. Godbillon, J., Gauron, S., and Metayer, J.P. High-performance liquid chromatographic determination of diclofenac and its monohydroxylated metabolities in biological fluids. Journal of Chromatography 27, 151-159 (1985).
[4]. Yamakazi, R., Kawai, S., Matsumoto, T., et al. Hydrolytic activity is essential for aceclofenac to inhibit cyclooxygenase in rheumatoid synovial cells. Journal of Pharmacology and Experimental Therapeutics 289(2), 676-681 (1999)
| Cas No. | 64118-84-9 | SDF | |
| 别名 | 4′-羟基双氯芬酸 | ||
| 化学名 | 2-[(2,6-dichloro-4'-hydroxyphenyl)amino]-benzeneacetic acid | ||
| Canonical SMILES | OC(=O)Cc1ccccc1Nc1c(Cl)cc(O)cc1Cl | ||
| 分子式 | C14H11Cl2NO3 | 分子量 | 312.2 |
| 溶解度 | 30mg/mL in ethanol, or in DMSO, or in DMF | 储存条件 | Store at -20°C, protect from light, stored under nitrogen |
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.2031 mL | 16.0154 mL | 32.0307 mL |
| 5 mM | 0.6406 mL | 3.2031 mL | 6.4061 mL |
| 10 mM | 0.3203 mL | 1.6015 mL | 3.2031 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。
A multi-biomarker approach to assess toxicity of diclofenac and 4-OH diclofenac in Mytilus trossulus mussels - First evidence of diclofenac metabolite impact on molluscs
Environ Pollut 2022 Dec 15;315:120384.PMID:36223851DOI:10.1016/j.envpol.2022.120384.
Although the presence of pharmaceuticals in the environment is an issue widely addressed in research over the past two decades, still little is known about their transformation products. However, there are indications that some of these chemicals may be equally or even more harmful than parent compounds. Diclofenac (DCF) is among the most commonly detected pharmaceuticals in the aquatic environment, but the potential effects of its metabolites on organisms are poorly understood. Therefore, the present study aimed to evaluate and compare the toxicity of DCF and its metabolite, 4-hydroxy Diclofenac (4-OH DCF), in mussels using a multi-biomarker approach. Mytilus trossulus mussels were exposed to DCF and 4-OH DCF at 68.22 and 20.85 μg/L (measured concentrations at day 0), respectively, for 7 days. In our work, we showed that both tested compounds have no effect on most of the enzymatic biomarkers tested. However, it has been shown that their action can affect the protein content in gills and also be reflected through histological markers. ENVIRONMENTAL IMPLICATION: Studies in recent years clearly prove that pharmaceuticals can negatively affect aquatic organisms. In addition to parent compounds, metabolites of pharmaceuticals can also be a significant environmental problem. In the present work, the effects of diclofenac and its main metabolite, 4-hydroxy Diclofenac, on marine mussels were evaluated. Both compounds showed negative effects on mussels, which was primarily observed through histological changes. The present study therefore confirms that not only diclofenac, but also its main metabolite can have negative effects on aquatic organisms.
Long-term stability of diclofenac and 4-hydroxydiclofenac in the seawater and sediment microenvironments: Evaluation of biotic and abiotic factors
Environ Pollut 2022 Jul 1;304:119243.PMID:35381302DOI:10.1016/j.envpol.2022.119243.
Studies in recent years have shown that significant amounts of diclofenac (DCF) and its metabolites are present in marine coastal waters. Their continuous flow into the environment may be associated with numerous negative effects on both fauna and flora. Although more and more is known about the effects of pharmaceuticals on marine ecosystems, there are still many issues that have not received enough attention, but are essential for risk assessment, such as long term stability. Furthermore, interaction of pharmaceuticals with sediments, which are inhabited by rich microbial, meiofaunal and macrobenthic communities need investigation. Therefore, we undertook an analysis of the stability of DCF and its metabolite, 4-hydroxy Diclofenac, in seawater and sediment collected from the brackish environment of Puck Bay. Our 29-day experiment was designed to gain a better understanding of the fate of these compounds under experimental conditions same as near the seafloor. Diclofenac concentration decreased by 31.5% and 20.4% in the tanks with sediment and autoclaved sediment, respectively during 29-day long experiment. In contrast, the concentration of 4-OH diclofenac decreased by 76.5% and 90.2% in sediment and autoclaved sediment, respectively. The concentration decrease of both compounds in the sediment tanks resulted from their sorption in the sediment and biodegradation. Obtained results show that marine sediments favour DCF and 4-OH DCF removal from the water column.