1418747-15-5

AZ3976 is a potent plasminogen activator inhibitor type 1 (PAI-1) inhibitor with an IC50?value of 26 μM?in an enzymatic chromogenic assay. AZ3976 is active with an IC50?of 16 μM in a plasma clot lysis assay.?AZ3976 does not bind to active PAI-1 but bound reversibly to latent PAI-1. AZ3976 inhibits PAI-1 by enhancing the latency transition of active PAI-1. AZ3976 displays profibrinolytic activities in a human plasma clot lysis assay[1].

[1] Ola Fjellstr?m, et al. Characterization of a small molecule inhibitor of plasminogen activator inhibitor type 1 that accelerates the transition into the latent conformation. J Biol Chem. 2013 Jan 11;288(2):873-85. DOI:10.1074/jbc.M112.371732