FR 122047 HYDROCHLORIDE

Description

FR122047 is a selective inhibitor of COX-1. The IC₅₀ values for inhibition of human COX-1 and COX-2 are 0.028 and 65 μM, respectively. In human platelet-rich plasma, FR122047 inhibits arachidonic acid, collagen, and ADP-induced platelet aggregation with an IC₅₀ of 180-200 nM, which is nearly 100 times more potent than aspirin. Unlike aspirin, FR122047 does not induce gastric damage upon oral administration at doses (100 mg/kg) far in excess of the dose needed for complete suppression of platelet COX-1. In some models of inflammation, such as collagen-induced arthritis in the rat, FR122047 has an anti-inflammatory effect, implying a role for COX-1 in these models.

Uses

FR 122047 Hydrochloride is a selective cyclooxygenase-1 (Cox-1) inhibitor.

Biological Activity

Selective cyclooxygenase-1 (COX-1) inhibitor (IC 50 values are 0.028 and 65 μ M for COX-1 and COX-2 respectively). Antiplatelet, analgesic and anti-inflammatory following oral administration in vivo .

storage

Desiccate at +4°C