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Diclofenac amide

A prodrug form of diclofenac

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Diclofenac amide的二维码
  • 库存: 现货
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  • 50mg
    ¥575.00
    460.00
    - +
  • 100mg
    ¥1100.00
    880.00
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  • 500mg
    ¥4587.00
    3670.00
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  • 1g
    ¥8050.00
    6440.00
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  • 货号: ajcx22266
  • CAS: 15362-40-0
  • 别名: 1-(2,6-二氯苯基)-1,3-二氢-2H-吲哚-2-酮
  • 分子式: C14H9Cl2NO
  • 分子量: 278.1
  • 纯度: >98%
  • 溶解度: DMF: >50mg/mL,DMSO: >40mg/mL,Ethanol: >35mg/mL,PBS (pH 7.2): >9mg/mL
  • 储存: Store at -20°C
  • 库存: 现货

Background

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)

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