UK-396082 is a potent and selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (activated TAFI, TAFIa) with Ki of 10 nM.
UK-396082 displays excellent selectivity over plasma carboxypeptidase N (>1,000-fold).
UK-396082 exhibits antithrombotic efficacy in a rabbit model of venous thrombosis, yet has no effect on surgical bleeding in the rabbit.
UK-396082 possesses excellent preclinical and clinical pharmacokinetic profile, and shows potential for the treatment of thrombosis and other fibrin-dependent diseases in humans.
