FR-188582

FR-188582 is a highly selective inhibitor of cyclooxygenase (COX)-2, with an IC₅₀ value of 17 nM. IC50 & Target: IC50: 17 nM (COX-2)^[1] In Vitro: In a recombinant human cyclooxygenase (COX) enzyme activity, FR-188582 (FR188582) inhibits COX-2 with an IC₅₀ value of 17 nM, and the inhibition of prostaglandin (PG) E2 formation by FR188582 isover 6000 times more selective for COX-2 than COX-1^[1]. In Vivo: Oral administration of FR-188582 (0.01-3.2 mg/kg) reverses paw edema in adjuvant arthritic rats and shows a therapeutic effect in a dose-dependent manner with ED₅₀ values (95% C.L.) of 0.074 (0.00021-0.53) and 0.063 (0.0039-0.31) mg/kg for adjuvant-injected paws and adjuvant-uninjected paws, respectively. The anti-inflammatory effect of FR-188582 (FR188582) is threefold more potent than that of Indomethacin with ED₅₀ values (95% C.L.) of 0.24 (0.047-1.8) and 0.20 (0.021-0.79) mg/kg for adjuvant-injected paws and adjuvant-uninjected paws, respectively^[1].