Bioactivity | AChE-IN-29, 3-OH pyrrolidine derivative, is an cholinesterase (ChE) inhibitor. AChE-IN-29 has cholinesterase inhibitory activity for hAChE, eeAChE and eqBChE with IC50 values of 0.25 μM, 0.23 μM and 0.72 μM, respectively. AChE-IN-29 can be used for the research of Alzheimer's disease[1]. |
Target | IC50: 0.25 μM (hAChE); 0.23 μM (eeAChE); eqBChE (0.72 μM); 24.12 μM (in DPPH assay) |
Invitro | AChE-IN-29 (VA10) 可有效抑制 AChE、BChE 和 Aβ1-42[1]。AChE-IN-29 对 hAChE、eeAChE 和 eqBChE 具有胆碱酯酶抑制活性,IC50 值分别为 0.25 μM、0.23 μM 和 0.72 μM[1]。AChE-IN-29 具有显著的抗氧化活性,在 DPPH 试验中的 IC50 值为 24.12 μM[1]。AChE-IN-29(5 μM、10 μM、20 μM)可抑制自身诱导的 Aβ1-42 聚集以及 hAChE 诱导的 Aβ1-42 聚集[1]。 Cell Viability Assay[1] Cell Line: |
In Vivo | AChE-IN-29 (VA10) (p.o.; 2.5, 5, and 10 mg/kg) 通过抑制 AChE 活性改善记忆和认知功能障碍[1]。AChE-IN-29 (p.o.; 10 mg/kg) 恢复海马区的细胞密度[1]。 Animal Model: |
Name | AChE-IN-29 |
Formula | C18H19BrN2O2 |
Molar Mass | 375.26 |
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]. Bhanukiran K,et al. Discovery of multi-target directed 3-OH pyrrolidine derivatives through a semisynthetic approach from alkaloid vasicine for the treatment of Alzheimer's disease. Eur J Med Chem. 2023;249:115145. |