ASP-6537 (FK 881, FR 122047) is a novel potent, selective, reversible cyclooxygenase-1 (COX-1) inhibitor with IC50 of 4.9 nM.
ASP-6537 displays 650-fold selectivity over COX-2 (IC50=3.2 uM).
ASP-6537 dose dependently inhibits carrageenan-induced paw edema (ED30=22 mg/kg) and paw swelling associated with adjuvant arthritis (ED50=17 mg/kg) in rats.
ASP-6537 also inhibits TXA2 production more selectively than aspirin in in vitro and in vivo, exerts potent antithrombotic effect in rats.
