tcsc2163 Naproxen

Naproxen is a COX-1 and COX-2 inhibitor with IC₅₀s of 8.72 and 5.15 μM, respectively in cell assay.

IC50 & Target: IC50: 8.72 μM (COX-1), 5.15 μM (COX-2)^[1]

In Vitro: Naproxen etemesil is a lipophilic, non-acidic, inactive prodrug of naproxen that is hydrolysed to pharmacologically active Naproxen once absorbed. Naproxen is a well known nonsteroidal anti-inflammatory drug. Naproxen is approximately equipotent inhibitor of COX-1 and COX-2 in intact cells with IC₅₀s of 2.2 μg/mL and 1.3 μg/mL, respectively^[1].

In Vivo: Naproxen exerts an anti-inflammatory and antifibrotic effect in mouse model of bleomycin-induced lung fibrosis. Naproxen also downregulates TGF-β levels and Smad3/4 complex formation^[2]. Naproxen is shown to inhibit the time-courses of pain, fever and PGE2 with similar potencies (IC₅₀=27, 40, 13 μM)^[3].