Plasminogen activator inhibitor-1 (PAI-1) inhibitor (IC50
= 2.7 μ
M). Induces vascular smooth muscle cell apoptosis in vitro
and reduces carotid artery neointimal formation in a rat vascular injury model. Promotes thrombolysis in rat and dog models of acute arterial thrombosis. Orally available.
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A small molecule PAI-1 functional inhibitor attenuates neointimal hyperplasia and vascular smooth muscle cell survival by promoting PAI-1 cleavage.
Simone et al.
Tiplaxtinin, a novel, orally efficacious inhibitor of plasminogen activator inhibitor-1: design, synthesis, and preclinical characterization.
Elokdah et al.