Diclofenac amide
(Synonyms: 1-(2,6-二氯苯基)-1,3-二氢-2H-吲哚-2-酮) 目录号 : GC47212
A prodrug form of diclofenac
Cas No.:15362-40-0
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
Diclofenac amide is a prodrug form of the non-steroidal anti-inflammatory drug (NSAID) diclofenac .1 It decreases paw thickness in a rat model of carrageenan-induced paw edema when administered at a dose of 100 μmol/kg and decreases acetic acid-induced writhing in mice at 100 μmol/kg.2 Diclofenac amide has reduced ulcerogenicity in rats compared to diclofenac. It is also a degradation product of diclofenac resulting from photo-transformation or spontaneous cyclization in strongly acidic pH conditions.3,4 Diclofenac amide has been used as a synthetic intermediate in the synthesis of compounds with anticancer activity as well as compounds with COX-1, COX-2, and/or 5-lipoxygenase (5-LO) inhibitory activity.5,6
1.Santos, J., Moreira, V., Campos, M.L., et al.Pharmacological evaluation and preliminary pharmacokinetics studies of a new diclofenac prodrug without gastric ulceration effectInt. J. Mol. Sci.13(11)15305-15320(2012) 2.Chung, M.C., dos Santos, J.L., Oliveira, E.V., et al.Synthesis, ex vivo and in vitro hydrolysis study of an indoline derivative designed as an anti-inflammatory with reduced gastric ulceration propertiesMolecules14(9)3187-3197(2009) 3.Epold, I., Dulova, N., and Trapido, M.Degradation of diclofenac in aqueous solution by homogeneous and heterogeneous photolysisJ. Environ. Eng. Ecol. Sci.1(3)1-8(2012) 4.Mertz, N., Larsen, S.W., Kristensen, J., et al.Long-acting diclofenac ester prodrugs for joint injection: Kinetics, mechanism of degradation, and in vitro release from prodrug suspensionJ. Pharm. Sci.105(10)3079-3087(2016) 5.Kaur, M., and Singh, P.Targeting tyrosine kinase: Development of acridone - pyrrole - oxindole hybrids against human breast cancerBioorg. Med. Chem. Lett.29(1)32-35(2018) 6.Shaveta, Singh, A., Kaur, M., et al.Rational design, synthesis and evaluation of chromone-indole and chromone-pyrazole based conjugates: Identification of a lead for anti-inflammatory drugEur. J. Med. Chem.77185-192(2014)
| Cas No. | 15362-40-0 | SDF | |
| 别名 | 1-(2,6-二氯苯基)-1,3-二氢-2H-吲哚-2-酮 | ||
| Canonical SMILES | ClC1=C(N2C(CC3=C2C=CC=C3)=O)C(Cl)=CC=C1 | ||
| 分子式 | C14H9Cl2NO | 分子量 | 278.1 |
| 溶解度 | DMF: >50mg/mL,DMSO: >40mg/mL,Ethanol: >35mg/mL,PBS (pH 7.2): >9mg/mL | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.5958 mL | 17.9791 mL | 35.9583 mL |
| 5 mM | 0.7192 mL | 3.5958 mL | 7.1917 mL |
| 10 mM | 0.3596 mL | 1.7979 mL | 3.5958 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。