A PAI-1 inhibitor
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PAZ-417

Item No. 42122

Technical Information
Formal Name
1-[[4-(1,1-dimethylethyl)phenyl]methyl]-5-(3-methylphenyl)-α-oxo-1H-indole-3-acetic acid
CAS Number
481629-87-2
Synonyms
  • Aleplasinin
Molecular Formula
C28H27NO3
Formula Weight
Purity
≥95%
Formulation
A solid
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
O=C(C(C1=CN(CC2=CC=C(C(C)(C)C)C=C2)C3=CC=C(C4=CC(C)=CC=C4)C=C13)=O)O
InChi Code
InChI=1S/C28H27NO3/c1-18-6-5-7-20(14-18)21-10-13-25-23(15-21)24(26(30)27(31)32)17-29(25)16-19-8-11-22(12-9-19)28(2,3)4/h5-15,17H,16H2,1-4H3,(H,31,32)
InChi Key
HSXLMAFNWCSZGP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    PAZ-417 is an inhibitor of plasminogen activator inhibitor 1 (PAI-1; IC50 = 655 nM).1 It is selective for PAI-1 over tissue-type plasminogen activator (tPA) and plasminogen, as well as a panel of 40 neurotransmitter, endocrine, and enzymatic targets, at 10 µM. PAZ-417 (5 µM) enhances cleavage of monomeric and oligomeric amyloid-β (1-42) (Aβ42) in a cell-free assay. In vivo, PAZ-417 (20 mg/kg) reduces plasma Aβ40 and brain Aβ40 and Aβ42 levels in the Tg2576 transgenic mouse model of Alzheimer’s disease. It also reverses cognitive deficits in the same model when administered at doses of 30 and 100 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jacobsen, J.S., Comery, T.A., Martone, R.L., et alEnhanced clearance of Aβ in brain by sustaining the plasmin proteolysis cascade. Proc. Natl. Acad. Sci. USA 105(25), 8754-8759 (2008).