Bioactivity | AChE/Aβ-IN-2 (compound 33) is a potent and orally active inhibitor of acetylcholinesterase (AChE) with IC50 of 135 nM, as well as an antagonist of NMDA receptor (GluN1-1b/GluN2B subunit combination) with IC50 of 5.054 μM. AChE/Aβ-IN-2 also inhibits Aβ aggregation and shows good blood-brain barrier permeability. AChE/Aβ-IN-2 improves cognitive and spatial memory impairment in rats model[1]. |
Target | IC50: 135 nM (AChE), 5.054 μM (NMDA receptor, GluN1-1b/GluN2B subunit) |
Invitro | AChE/Aβ-IN-2 (compound 33) (5-20 μM; 48 h) 抑制 Aβ1-42 (10 μM) 聚集[1]。 0 --> AChE/Aβ-IN-2 相关抗体: |
In Vivo | AChE/Aβ-IN-2 (compound 33) (10 mg/kg/d; po; 7 days) 抑制 Aβ1-42 诱导的大鼠记忆缺陷,减少 Morris 水迷宫平台区的停留时间[1]。 |
Name | AChE/Aβ-IN-2 |
Formula | C20H25ClN4 |
Molar Mass | 356.89 |
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]. Gutti G, et al. Discovery of triazole-bridged aryl adamantane analogs as an intriguing class of multifunctional agents for treatment of Alzheimer's disease. Eur J Med Chem. 2023 Nov 5;259:115670. |