| 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. |