| Bioactivity | MAO-B-IN-21 is an excellent MAO-B inhibitor with antioxidant activity and anti-Aβ aggregation activity. MAO-B-IN-21 also exhibits metal-ion chelating ability, anti-neuroinflammation (NO, TNF-α), neuroprotective activity and BBB permeability. MAO-B-IN-21 significantly improves the memory and cognitive impairment in Aβ1-42 induced Alzheimer's disease mice model[1]. |
| Invitro | MAO-B-IN-21 (37.5 μM 甲醇溶液) 阻断 Cu2+ 诱导的 ROS 产生，这是由于它的金属螯合特性和/或其抗氧化能力，而能够从 Cu2+-抗坏血酸氧化还原系统捕获自由基[1]。MAO-B-IN-21 (25 μM; 24 h; 37 ℃) 抑制自诱导的 Aβ1-42 聚集并分解自诱导的 Aβ1-42 原纤维[1]。MAO-B-IN-21 (2.5-25 μM；24 小时) 抑制 LPS 刺激的 BV-2 小胶质细胞中 ROS 的产生[1]。 |
| In Vivo | MAO-B-IN-21 (30 mg/kg；ig；单次剂量) 可以在 Balb/C 小鼠中轻松透过血脑屏障[1]。MAO-B-IN-21 (8 mg/kg 和 32 mg/kg；ig；单剂量) 缩短逃逸潜伏期 (ELT)，降低 Aβ1-42 水平，表明 Aβ 诱导的 AD 小鼠模型的学习和记忆能力得到改善 [1]。在 Balb/C 小鼠中的药代动力学分析[1]Tissue |
| Name | MAO-B-IN-21 |
| Formula | C24H25ClN2O4 |
| Molar Mass | 440.92 |
| 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]. Cong S, et al. Discovery of novel 5-(2-hydroxyphenyl)-2-phthalide-3(3H)-pyrazolones as balanced multifunctional agents against Alzheimer's disease. Eur J Med Chem. 2023 Mar 15;250:115216. |