| Bioactivity | AChE/BChE-IN-23 (Compound 6e) is an AChE/BChE inhibitor (IC50: 0.91 μM, 1.19 μM and 1.01 μM for hAChE, eq BChE and hBChE, respectively). AChE/BChE-IN-23 has antioxidant activity and inhibits Aβ1-42 and Tau protein aggregation. AChE/BChE-IN-23 also inhibits microglial activation by reducing ROS release and mitochondrial injury. AChE/BChE-IN-23 suppresses NLRP3 inflammasome and pro-inflammatory cytokines in human microglial cells. AChE/BChE-IN-23 also reverses the Scopolamine (HY-N0296)-induced memory impairment in mice model[1]. |
| Invitro | AChE/BChE-IN-23 会导致碘化丙啶 (对 AChE 酶有亲和力) 移位 (5 μM，2.06%；10 μM，11.78%；20 μM，14.47%；50 μM，27.53%)[1].。AChE/BChE-IN-23 具有抗氧化作用 (20 μM;对DPPH清除率为47.30%，IC50:15.17 μM) [1].。AChE/BChE-IN-23 (3.125 μM, 72 h) 能有效抑制 Aβ1-42 (12.5 μM) 的聚集[1].。AChE/BChE-IN-23 (1.125 μM, 72 h) 能有效抑制 Tau (5 μM) 的聚集[1].。AChE/BChE-IN-23 (1-20 μM, 24 h) 对 PC-12 细胞没有毒性[1].。AChE/BChE-IN-23 (12.5 μM, 24 h) 通过减少 ROS 的释放和恢复线粒体膜电位抑制小胶质细胞的激活[1]。AChE/BChE-IN-23 (12.5 μM, 24 h) 通过抑制小胶质细胞中炎性小体和 NF-κB 的激活发挥抗炎作用[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> AChE/BChE-IN-23 相关抗体: Western Blot Analysis[1] Cell Line: |
| In Vivo | AChE/BChE-IN-23 (10 mg/kg，腹腔注射，14 天) 通过增强 AD 小鼠的空间记忆和认知记忆，逆转了东莨菪碱诱导的阿尔兹海默症[1].。AChE/BChE-IN-23 (2000 mg/kg，灌胃，14 天) 对 Swiss albino 小鼠无毒性，包括与急性毒性相关的体重增加、行为异常、抽搐、震颤或腹泻[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C19H21N5O3 |
| Molar Mass | 367.40 |
| 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]. Shankar G, et al. Discovery of novel substituted (Z)-N'-hydroxy-3-(3-phenylureido)benzimidamide derivatives as multifunctional molecules targeting pathological hallmarks of Alzheimer's disease. Eur J Med Chem. 2024;280:116959. |