Aceclofenac

Aceclofenac is a non-steroidal anti-inflammatory drug (NSAID) and a derivative of diclofenac (Item Nos. 22983 | 70680).¹ Aceclofenac inhibits the production of prostaglandin E₂ (PGE₂; Item No. 14010) and thromboxane B₂ (TXB₂; Item No. 19030) by 25 and 30%, respectively, in cell-free assays when used at concentrations of 10 and 100 µM, respectively. It selectively inhibits COX-2 in isolated whole blood (IC₅₀s = 0.8 and >100 µM for COX-2 and COX-1, respectively) and inhibits the production of PGE₂ in patient-derived human rheumatoid synovial cells (IC₅₀s = 1.9-29.4 nM).^1,2 Aceclofenac reduces IL-1β-induced increases in IL-6 production by 21 and 43% in cultured chondrocytes without and with osteoarthritic lesions, respectively, when used at a concentration of 30 μM.¹ Aceclofenac inhibits carrageenan-induced paw edema (ED₅₀ = 3.6 mg/kg) and abscess formation (ED₃₀ = 1.1 mg/kg) in rats.³ It also inhibits an increase in joint diameter in a rat model of arthritis induced by complete Freund’s adjuvant (CFA).⁴

WARNING This product is not for human or veterinary use.

1. Henrotin, Y., de Leval, X., Mathy-Hartet, M., et al. In vitro effects of aceclofenac and its metabolites on the production by chondrocytes of inflammatory mediators. Inflamm. Res. 50(8), 391-399 (2001).

2. Yamazaki, 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).

3. Grau, M., Guasch, J., Montero, J.L., et al. The pharmacological profile of aceclofenac, a new nonsteroidal antiinflammatory and analgesic drug. Agents Actions Suppl. 32, 125-129 (1991).

4. Poorvashree, J., and Suneela, D. Novel drug delivery of dual acting prodrugs of hydroxychloroquine with aryl acetic acid NSAIDs: Design, kinetics and pharmacological study. Drug Deliv. Transl. Res. 7(5), 709-730 (2017).