4'-Hydroxy diclofenac 

4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac (HY-15036) by cytochrome P450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties^[1][2].

A single oral administration of Diclofenac to humanized mice, the unchanged drug in plasma peaks at 0.25 hour and then declines with a half-life (t_1/2) of 2.4 hours. 4'-Hydroxy diclofenac also peaks at 0.25 hour and is undetectable within 24 hours. The plasma concentration of unchanged 4'-Hydroxy diclofenac peaks at 0.25 hour and declines rapidly in Humanized chimeric mice received of 4'-Hydroxy diclofenac (10 mg/kg; a single oral)^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

312.15

Solid

C₁₄H₁₁Cl₂NO₃

64118-84-9

O=C(O)CC1=CC=CC=C1NC2=C(Cl)C=C(O)C=C2Cl

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

• [1]. J Shimamoto, et al. Lack of Differences in Diclofenac (A Substrate for CYP2C9) Pharmacokinetics in Healthy Volunteers With Respect to the Single CYP2C9*3 Allele. Eur J Clin Pharmacol. 2000 Apr;56(1):65-8.  [Content Brief]

  [2]. Hidetaka Kamimura, et al. Formation of the Accumulative Human Metabolite and Human-Specific Glutathione Conjugate of Diclofenac in TK-NOG Chimeric Mice With Humanized Livers. Drug Metab Dispos. 2015 Mar;43(3):309-16.  [Content Brief]