| Bioactivity | BuChE-IN-11 (Compound 3b-1) 是一种 BuChE 选择性抑制剂，其中hBuChE 的 IC50 为0.44 μM。PARP7-IN-22血脑屏障透过性高，具有自由基清除作用因此具有强大的抗氧化活性。BuChE-IN-11可以与胆碱结合位点、乙酰结合位点和外周阴离子位点相互作用，表现出亚微摩尔级别的BuChE抑制活性并且防止β-淀粉样蛋白 (Aβ) 的自聚集。BuChE-IN-11有望用于阿尔兹海默疾病领域研究[1]。 |
| Invitro | BuChE-IN-11 (Compound 3b-1) (0.1-1 µM, 120 min) 具有极强抗氧化活性[1]。BuChE-IN-11 (20 μM, 48h)具有抑制 αβ1-42 聚集的作用[1]。低于25 μM的BuChE-IN-11 (12.5-100 μM for PC12, 25-100 μM for AML12, 24h) 对PC12和AML12细胞没有显著毒性[1]。BuChE-IN-11 (18h) 显示出良好的血脑屏障渗透性 (CNS+)，可以穿过血脑屏障[1]。BuChE-IN-11 被预测具有高胃肠道吸收活性和低心脏毒性风险[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> BuChE-IN-11 相关抗体: Cell Cytotoxicity Assay[1] Cell Line: |
| Formula | C28H27FN4O2 |
| Molar Mass | 470.54 |
| 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]. Zeng X, et al. Design, synthesis, and activity evaluation of novel multitargeted l‐tryptophan derivatives with powerful antioxidant activity against Alzheimer's disease[J]. Archiv der Pharmazie, 2024: e2300603. |