| Bioactivity | BuChE-IN-7 is a highly selective inhibitor of hBuChe and eqBuChE with IC50 values of 40 nM, 80 nM respectively. BuChE-IN-7 can promote cognitive with blood-brain penetration and improves situational and phobic memory, showing preference for new things[1]. |
| Invitro | BuChE-IN-7 (compound (R)-29) (10 µM；5 min) 抑制 eqBuChE、hBuChE 的 IC50 值分别为 0.08 µM、0.04 µM[1]。BuChE-IN-7 (1、10、50 和 100 µM；72 h) 在 HepG2 细胞系中具有肝毒性，IC50 值为 2.85 µM。BuChE-IN-7 减弱了细胞活性，对 CYP3A4 的影响较弱[1]。 |
| In Vivo | BuChE-IN-7 (compound (R)-29) (10 mg/kg 和 30 mg/kg；腹腔注射；单剂量) 对由东莨菪碱 (HY-N0296) 引起的健忘症小鼠模型的记忆改善功能没有作用，能透过血脑屏障[1]。BuChE-IN-7 (10 mg/kg；腹腔注射；每日一次，共 6 天) 没有显著改善由东莨菪碱引起的小鼠学习缺陷[1]。BuChE-IN-7 (15 mg/kg 和 30 mg/kg；腹腔注射；单剂量) 显著促进认知并改善了小鼠的情境性、恐惧性记忆，表现出对新事物的偏好[1]。 |
| Name | BuChE-IN-7 |
| Formula | C25H34N2O2 |
| Molar Mass | 394.55 |
| 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]. Panek D, et al. Discovery of new, highly potent and selective inhibitors of BuChE - design, synthesis, in vitro and in vivo evaluation and crystallography studies. Eur J Med Chem. 2023 Jan 18;249:115135. |