481629-87-2
Chemical Structure
Aleplasinin
Synonym(s): PAZ-417
- CAS No.: 481629-87-2
- Formula:C28H27NO3
- Molecular Weight:425.52
IUPAC Name: 2-(1-(4-(tert-butyl)benzyl)-5-(m-tolyl)-1H-indol-3-yl)-2-oxoacetic acid
InChIKey: HSXLMAFNWCSZGP-UHFFFAOYSA-N
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
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Aleplasinin | 99.16% | 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. | ||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
