| Bioactivity | hAChE-IN-8 (Compound S-12) is a orally effective and selective inhibitor of hAChE (IC50=0.486 μM). hAChE-IN-8 also inhibits BACE-1 (IC50=0.542 μM), and does not inhibit Dyrk1A (IC50>10 μM). hAChE-IN-8 can reduce Aβ aggregation, has good blood-brain barrier penetration. hAChE-IN-8 is mainly used in Alzheimer's disease research[1]. |
| Invitro | hAChE-IN- 8 (10-80 μM; 72 h) 在高浓度下对 SH-SY5Y 神经细胞无毒性[1]。hAChE-IN- 8 (40 μM; 72 h) 在 Aβ1-42 引起的氧化应激中保护 SH-SY5Y 细胞存活率显著提高，细胞形态恢复正常[1]。hAChE-IN- 8 (5-20 μM; 48 h) 显示出显著的抗 Aβ 聚集活性[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> hAChE-IN-8 相关抗体: |
| In Vivo | hAChE-IN- 8 (500,1000 mg/kg; p.o.; single dose) 在高剂量下,所有大鼠在 14 天观察期内未显示任何毒性或异常反应[1]。hAChE-IN- 8 (2.5-10 mg/kg; p.o.; single dose) 剂量依赖性下改善了东莨菪碱 (HY-N0296) 诱导的记忆丧失。在东莨菪碱诱导的氧化应激中表现出抗氧化潜力，并能恢复 ACh 和 AChE 水平[1]。hAChE-IN- 8 (10 mg/kg; p.o.;once daily for 9 days) Aβ1-42 诱导的 AD 模型中表现出显著的认知改善效果。显著降低 AD 相关蛋白水平[1]。hAChE-IN- 8 (10-200 μM) 添加到果蝇的培养基中，在较低浓度下对果蝇无明显毒性，但在高浓度下表现出一定的毒性[1]。hAChE-IN- 8 (10-20 μM) 在果蝇 AD 模型中有效恢复了 Aβ42 诱导的眼部表型变化，表现出显著的神经保护作用[1]。hAChE-IN- 8 (5-50 μM) 在较低浓度下对幼虫细胞具有较高的存活率，但在高浓度下细胞存活率显著下降，表现出一定的细胞毒性[1]。 Wistar 大鼠中的药代动力学分析[1] Route |
| Formula | C25H22N4O4 |
| Molar Mass | 442.47 |
| 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]. Waiker DK, et al. Design, synthesis, and biological evaluation of some 2-(3-oxo-5,6-diphenyl-1,2,4-triazin-2(3H)-yl)-N-phenylacetamide hybrids as MTDLs for Alzheimer's disease therapy. Eur J Med Chem. 2024 May 5;271:116409. |