PeptideDB

AChE/BChE-IN-1

CAS: 2720624-42-8 F: C32H35ClN6O3 W: 587.11

AChE/BChE-IN-1 is a potent and brain-penetrant dual inhibitor of Acetylcholinesterase and Butyrylcholinesterase, with IC
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Bioactivity AChE/BChE-IN-1 is a potent and brain-penetrant dual inhibitor of Acetylcholinesterase and Butyrylcholinesterase, with IC50s of 1.06 and 7.3 nM for hAChE and hBChE, respectively. AChE/BChE-IN-1 also has antioxidant activity. AChE/BChE-IN-1 can be used for the research of Alzheimer’s disease[1].
Target IC50: 1.06 nM (hAChE); 7.3 nM (hBChE)
Invitro AChE/BChE-IN-1 (compound 5i) is notactive against hBACE-1 at the tested concentration (1 μM)[1].AChE/BChE-IN-1 scavenges the 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical, with an IC50 of 92.0 μM[1].
In Vivo AChE/BChE-IN-1 (2 mg/kg; i.p. 3 times per week for 4 weeks) rescues learning and memory impairments, delays the Alzheimer-like pathology progression, improves basal synaptic efficacy, and significantly reduces hippocampal oxidative stress and neuroinflammation in 10 month-old APP/PS1 mice[1]. Animal Model:
Name AChE/BChE-IN-1
CAS 2720624-42-8
Formula C32H35ClN6O3
Molar Mass 587.11
Transport Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Reference [1]. Viayna E, et, al. Discovery of a Potent Dual Inhibitor of Acetylcholinesterase and Butyrylcholinesterase with Antioxidant Activity that Alleviates Alzheimer-like Pathology in Old APP/PS1 Mice. J Med Chem. 2020 Dec 28.