BChE-IN-13

BChE-IN-13 (Compound 17c) is an orally active, potent and selective Butyrylcholinesterase (BChE) inhibitor with IC50s of 0.22 and 0.016 μM for eqBChE and hBChE, respectively. BChE-IN-13 can improve memory and cognitive impairments, and be used in Alzheimer’s disease (AD) research[1].

Research Areas >> Neurological Disease

Signaling Pathways >> Neuronal Signaling >> AChE

IC50: 0.22 μM (eqBChE) 0.016 μM (hBChE)[1]

BChE-IN-13 (5-100 μM; 24 h) shows weak toxicity to SH-SY5Y, PC-12 and HT-22, and shows high mortality to BV2 cells[1]. BChE-IN-13 shows excellent blood brain barrier permeation using a parallel artificial membrane permeability assay experiment (PAMPA)[1]. Cell Cytotoxicity Assay[1] Cell Line: SH-SY5Y, PC12, BV2 and HT-22 cells Concentration: 5-100 μM Incubation Time: 24 hours Result: Showed cells viability more than 60% of SH-SY5Y, PC-12 and HT-22 even at 100 μM. Showed high mortality in BV2 cells, and reached half the mortality at 20 μM.

BChE-IN-13 (oral gavage; 15 mg/kg; once daily; 6 d) shows the improvement in memory and cognitive function in Aβ1-42 induced AD-like disorder mice[1]. Animal Model: ICR mice intracerebroventricularly (icv) injected with oligomerized Aβ1-42 Dosage: 15 mg/kg Administration: Oral gavage; 15 mg/kg; once daily; 6 days Result: Improved the memory and cognitive function, and showed a shorter latency compared with Donepezil.

[1]. Xin Lu, et al. Design, synthesis, and biological evaluation of aromatic tertiary amine derivatives as selective butyrylcholinesterase inhibitors for the treatment of Alzheimer's disease.