| Bioactivity | AChE-IN-14 (compound 5) is a potent cholinesterase inhibitor with IC50s of 0.46 , 0.48, and 0.44 μM for electric eel acetylcholinesterase (eeAChE), human recombinant acetylcholinesterase (hAChE), and equine serum butyrylcholinesterase (eqBuChE), respectively. AChE-IN-14 exhibits high affinity toward human H3 receptor (H3R; Ki= 159.8 nM). AChE-IN-14 can be used for the research of Alzheimer’s disease[1]. |
| Invitro | AChE-IN-14 (compound 5) has a good affinity to human H3 receptor with a Ki value of 159.8 nM in HEK293 cells[1].AChE-IN-14 has a high orally activity and cannot cross the blood-brain barrier[1].AChE-IN-14 (10 μM, 5 min) inhibits hAChE with an IC50 value of 0.48 μM and represents the non-competitive type of eeAChE (Ki = 176 nM) and eqBuChE (Ki = 281 nM) inhibition[1]. |
| Name | AChE-IN-14 |
| CAS | 2390042-05-2 |
| Formula | C28H35NO3 |
| Molar Mass | 433.58 |
| 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]. Marek Bajda, et al. Search for new multi-target compounds against Alzheimer's disease among histamine H3 receptor ligands. Eur J Med Chem. 2020 Jan 1;185:111785. |