Aleplastinin (PAZ-417) is an orally active, blood-brain barrier permeable, selective SERPINE1 ( PAI-1 ) inhibitor ( IC 50 =655 nM). Aleplastinin activates the tissue type plasminogen activator (tPA) / fibrinolysis cascade by inhibiting PAI-1 , thereby promoting the degradation of amyloid-β (Aβ) oligomers and monomers. Aleplastinin can significantly reduce plasma and brain Aβ levels, improve memory impairment, and reverse cognitive impairment. Aleplastinin can be used for research on Alzheimer's disease.
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