| Description |
BChE-IN-14 (compound 19c) is a selective butyrylcholinesterase (BChE) inhibitor with IC50s of 0.23 and 0.011 μM for eqBChE and hBChE, respectively. BChE-IN-14 shows good blood brain barrier permeation and primary cell safety. BChE-IN-14 is able to restore cognitive impairment in vivo, it can be used for the research of Alzheimer’s disease[1].
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| Related Catalog |
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| Target |
IC50: 0.23 μM (eqBChE), 0.011 μM (hBChE)[1]
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| In Vitro |
BChE-IN-14 (0.0001-100 μM) inhibits eqBChE from house serum and hBChE with IC50s of 0.23 and 0.011 μM, respectively[1].
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| In Vivo |
BChE-IN-14 (15 mg/kg; p.o. for Aβ1-42 injection days 3-8) affects memory and cognitive function in AD mice model[1]. Animal Model: ICR mice with oligomerized Aβ1-42 peptide injection[1] Dosage: 15 mg/kg Administration: Oral gavage; 15 mg/kg for Aβ1-42 injection days 3-8 Result: Improved memory and cognitive function in vivo and showed a shorter latency than donepezil.
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| References |
[1]. Lu X, et al. Design, synthesis, and biological evaluation of aromatic tertiary amine derivatives as selective butyrylcholinesterase inhibitors for the treatment of Alzheimer's disease. Eur J Med Chem. 2022 Sep 2;243:114729.
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