Items for "potency"

A novel inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) - Part I: Pharmacological characterization

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