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4'-Hydroxy diclofenac

Cat. No. M30414
4'-Hydroxy diclofenac Structure
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Quality Control & Documentation
Biological Activity

4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac by cytochrome P450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties.

Chemical Information
Molecular Weight 312.15
Formula C14H11Cl2NO3
CAS Number 64118-84-9
Form Solid
Solubility (25°C) DMSO 10 mg/mL (ultrasonic and warming and heat to 60°C)
Storage -20°C, protect from light, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Klaudia Świacka, et al. Environ Pollut. 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

[2] Klaudia Świacka, et al. Environ Pollut. Long-term stability of diclofenac and 4-hydroxydiclofenac in the seawater and sediment microenvironments: Evaluation of biotic and abiotic factors

[3] Helene Bouju, et al. J Hazard Mater. Elucidation of biotransformation of diclofenac and 4'hydroxydiclofenac during biological wastewater treatment

[4] H Bouju, et al. Water Sci Technol. The fate of 14C-radiolabelled diclofenac and 4'-hydroxydiclofenac in membrane bioreactor treatment of wastewater

[5] D Landsdorp, et al. Int J Clin Pharmacol Ther Toxicol. Pharmacokinetics of rectal diclofenac and its hydroxy metabolites in man

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