AChE/BChE/BACE-1-IN-1

AChE/BChE/BACE-1-IN-1 (Compound 4k) is an orally active inhibitor of AChE, BChE, and BACE-1 with IC50 values of 0.058, 0.082 and 0.115 μM against hAChE, hBChE and hBACE-1, respectively. AChE/BChE/BACE-1-IN-1 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-1 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: 0.058 μM (hAChE), 0.082 μM (hBChE), 0.115 μM (hBACE-1)[1]

AChE/BChE/BACE-1-IN-1 (Compound 4k) (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.