Biochem/Physiol Actions | A cell-permeable trisubstituted thiazole compound that acts as a potent and selective inhibitor of COX-1 (IC50 = 28 nM and 65 µM for human recombinant COX-1 and COX-2, respectively). Displays ~2,300 fold greater selectivity towards inhibition of COX-1 over COX-2. Reported to be orally active and display analgesic, anti-platelet and anti-inflammatory properties. A potent, cell-permeable, and selective inhibitor of COX-1 (IC50 = 28 nM; human recombinant COX-1). Does not significantly inhibit COX-2 (IC50 = 65 µM, human recombinant COX-2). Reported to be orally active and displays analgesic properties in chemical nociceptive animal models. Also reported to exhibit anti-inflammatory effects and suppress prostaglandin E2 and thromboxane 2 levels in collagen-induced arthritis in rats. Shown to be 100 times more potent than aspirin in inhibiting arachidonic acid- and collagen-induced human and guinea pig platelet aggregation. |
