Valdecoxib

Valdecoxib is a highly potent and selective inhibitor of COX-2, with IC₅₀s of 5 nM and 140 μM for COX-2 and COX-1, respeceively. Valdecoxib can be used in the research of arthritis and pain. IC50 & Target:IC50: 5 nM (COX-2), 140 μM (COX-1)^[1] In Vitro: Valdecoxib (Compound 2) is a highly potent, selective and orally active inhibitor of COX-2, with IC₅₀s of 5 nM and 140 μM for COX-2 and COX-1, respeceively^[1]. Valdecoxib (10, 100 µM) inhibits LPS-induced proliferation of endothelial cells and bFGF secretion in a dose-dependent manner. Valdecoxib stimulates VEGF formation via HMEC-1 under inflammatory conditions^[2]. In Vivo: Valdecoxib (Compound 2) shows potent oral activity in an acute antiinflammatory assay (rat carrageenan foot pad edema; ED₅₀ = 10.2 ± 1.4 mg/kg). Valdecoxib also has chronic antiinflammatory activity in the rat adjuvant arthritis model, with an ED₅₀ of 0.032 ± 0.002 mg/kg/day^[1]. Valdecoxib (10 mg/kg, i.p.) significantly attenuates the behavioral and biochemical (oxidative damage) alterations in chronic-stressed mice^[3].