Aleplasinin

Aleplastinin (PAZ-417) is an orally active, blood-brain barrier permeable, selective SERPINE1 (PAI-1) inhibitor (IC50=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[1][2].

Product Specifications

CAS Number

[481629-87-2]

Product Name Alternative

PAZ-417

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

Amyloid-β; PAI-1

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease; Neuronal Signaling

Applications

Neuroscience-Neurodegeneration

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/aleplasinin.html

Purity

99.59

Solubility

DMSO : 250 mg/mL (ultrasonic)

Smiles

O=C(O)C(C1=CN(CC2=CC=C(C(C)(C)C)C=C2)C3=C1C=C(C4=CC=CC(C)=C4)C=C3)=O

Molecular Formula

C28H27NO3

Molecular Weight

425.52

Precautions

H302, H315, H319

References & Citations

[1]Jacobsen JS, et al. Enhanced clearance of Abeta in brain by sustaining the plasmin proteolysis cascade. Proc Natl Acad Sci U S A. 2008 Jun 24;105 (25) :8754-9.|[2]Kellici TF, et al. Therapeutic Potential of Targeting Plasminogen Activator Inhibitor-1 in COVID-19. Trends Pharmacol Sci. 2021 Jun;42 (6) :431-433.