An active metabolite of diclofenac
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4-hydroxy Diclofenac

Item No. 10008518

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(2,6-dichloro-4'-hydroxyphenyl)amino]-benzeneacetic acid
CAS Number
64118-84-9
Molecular Formula
C14H11Cl2NO3
Formula Weight
312.2
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlPBS (pH 7.2): 5 mg/ml
λmax
271 nm
SMILES
OC(=O)Cc1ccccc1Nc1c(Cl)cc(O)cc1Cl
InChi Code
InChI=1S/C14H11Cl2NO3/c15-10-6-9(18)7-11(16)14(10)17-12-4-2-1-3-8(12)5-13(19)20/h1-4,6-7,17-18H,5H2,(H,19,20)
InChi Key
KGVXVPRLBMWZLG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $138

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    5 mg

    $516

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    10 mg

    $895

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    Product Description

    4-hydroxy Diclofenac is an active metabolite of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor diclofenac (Item Nos. 70680 | 22983).1 It is formed from diclofenac by the cytochrome P450 (CYP) isoform CYP2C9 in human liver microsomes.2 4-hydroxy Diclofenac inhibits COX activity (IC50 = 32 nM) and reduces prostaglandin E2 (PGE2; Item No. 14010) production (IC50 = 17 nM) in isolated human rheumatoid synovial cells.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. 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).

    2. Yasar, U., Eliasson, E., Forslund-Bergengren, C., et al. The role of CYP2C9 genotype in the metabolism of diclofenac in vivo and in vitro. Eur. J. Clin. Pharmacol. 57(10), 729-735 (2001).

    3. Yamakazi, R., Kawai, S., Matsumoto, T., et al. Hydrolytic activity is essential for aceclofenac to inhibit cyclooxygenase in rheumatoid synovial cells. J. Pharmacol. Exp. Ther. 289(2), 676-681 (1999).

    Product Citations

    Negoro, R., Tasaka, M., Deguchi, S., et al. Generation of HepG2 cells with high expression of multiple drug-metabolizing enzymes for drug discovery research using a PITCh system. Cells 11(10), 1677 (2022).

    Zhang, F., Liu, W., Huang, J., et al. Inhibition of drug-metabolizing enzymes by Jingyin granules: Implications of herb-drug interactions in antiviral therapy. Acta Pharm. Sin. 43(4), 1072-1081 (2022).