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AEP-IN-3 (compound 18) is an orally active, potent and brain penetrant asparagine endopeptidase (AEP) inhibitor, with an IC50 of 7.8 ± 0.9 nM. AEP-IN-3 can be used for Alzheimer’s Disease (AD) research[1]. | [in vivo]
AEP-IN-3 (compound 18) has a bioavailability of 83% and a T1/2[1].
AEP-IN-3 (20 mg/kg, orally, BID, for 5 days) shows significantly inhibited activity of AEP in brain in TauP301L transgenic mice[1]. | Animal Model: | Mice producing the 2N4R isoform of human Tau containing the P301L mutation in a
FVB/N genetic background (3.8 months old)[1] | | Dosage: | 20 mg/kg | | Administration: | Orally, BID with an interval of 7-8 h between doses for 5 days | | Result: | Showed significantly inhibited activity of AEP in brain, reduced formation of the Tau N368 fragment. The effect on total Tau is not significant. |
| [References]
[1] Krummenacher D, et al. Discovery of Orally Available and Brain Penetrant AEP Inhibitors. J Med Chem. 2023 Dec 28;66(24):17026-17043. DOI:10.1021/acs.jmedchem.3c01804 |
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