We have discovered a novel small-molecule (3-phosphinoylpropionic acid) inhibitor of activated thrombin activatable fibrinolysis inhibitor (TAFIa), BX 528, which had an IC 50 of 2 nM in an enzymatic assay and 50 nM in an in-vitro clot lysis assay, with 3,500- to 35,000-fold selectivity against other carboxypeptidases, such as CPN, CPZ and CPD, and 5- and 12-fold selectivity against CPE (CPH) and CPB, respectively...
Keywords: TAFI, carboxypeptidases, potency, selectivity, safety, pharmacokinetics
01/2007 | Thrombosis and Haemostasis, SchattauerThe prothrombin gene mutation G20210A is a common risk factor for thrombosis and has been reported to cause APC resistance...
Keywords: Protein C, prothrombin G20210A, TAFI, thrombin generation, thrombosis
04/2006 | Thrombosis and Haemostasis, SchattauerIn this study, the in-vitro fibrinolytic efficacy of Tenecteplase, Amediplase and scu-PA was investigated in different external lysis models by measuring the lysis of human plasma clots after the addition of the plasminogen activators (PAs) to the surrounding plasma...
Keywords: TAFI, plasminogen activator, fibrinolysis, thrombolysis, Amediplase, Tenecteplase
09/2006 | Thrombosis and Haemostasis, Schattauer