AChE/BChE/BACE-1-IN-2

AChE/BChE/BACE-1-IN-2 (Compound 4o) is an orally active inhibitor of AChE, BChE, and BACE-1 with IC50 values of 0.069, 0.127 and 0.097 μM against hAChE, hBChE and hBACE-1, respectively. AChE/BChE/BACE-1-IN-2 shows considerable PAS-AChE binding capability, excellent brain permeation, potential disassembly of Aβ aggregates, and neuroprotective activity against Aβ-induced stress. AChE/BChE/BACE-1-IN-2 has remarkable antioxidant potential[1].

Signaling Pathways >> Neuronal Signaling >> Beta-secretase

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> ROS

Research Areas >> Neurological Disease

Signaling Pathways >> Neuronal Signaling >> AChE

IC50: 0.069 μM (hAChE), 0.097 μM (hBACE-1), 0.127 μM (hBChE)[1]

AChE/BChE/BACE-1-IN-2 (Compound 4o) (0-10 mg/kg; p.o.) ameliorates cognitive dysfunction against the scopolamine-induced amnesia model in the Y-maze test[1].

[1]. Choubey PK, et al. Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer's disease. Bioorg Med Chem. 2020 Nov 15;28(22):115721.