Diclofenac amide (Synonyms: Diclofenac Lactam, 1-(2,6-Dichlorophenyl)oxindole, NSC 621845) |
| Catalog No.GC47212 |
A prodrug form of diclofenac
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 15362-40-0
Sample solution is provided at 25 µL, 10mM.
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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 | |
| Synonyms | Diclofenac Lactam, 1-(2,6-Dichlorophenyl)oxindole, NSC 621845 | ||
| Canonical SMILES | ClC1=C(N2C(CC3=C2C=CC=C3)=O)C(Cl)=CC=C1 | ||
| Formula | C14H9Cl2NO | M.Wt | 278.1 |
| Solubility | DMF: >50mg/mL,DMSO: >40mg/mL,Ethanol: >35mg/mL,PBS (pH 7.2): >9mg/mL | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)
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