PAZ-417

A PAI-1 inhibitor (IC50 = 655 nM), selective for PAI-1 over tPA and plasminogen, as well as a panel of 40 neurotransmitter, endocrine, and enzymatic targets, at 10 µM, enhances cleavage of monomeric and oligomeric Abeta42 in a cell-free assay at 5 µM, reduces plasma Abeta40 and brain Abeta40 and Abeta42 levels in the Tg2576 transgenic mouse model of Alzheimer's disease at 20 mg/kg, reverses cognitive deficits in the same model at 30 and 100 mg/kg. Formulation: A solid. InChI: 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). InChIKey: HSXLMAFNWCSZGP-UHFFFAOYSA-N. 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