AChE-IN-12 是一种有效的、具有血脑屏障 (BBB) 渗透性的乙酰胆碱酯酶 (AChE) 抑制剂,对大鼠 AChE 和电鳗 AChE 的IC50分别为 0.41 μM 和 1.88 μM。AChE-IN-12 还是一种良好的抗氧化剂 (ORAC = 3.3eq)、选择性金属螯合剂和huMAO-B 抑制剂 (IC50= 8.8 μM)。AChE-IN-12 对 Cu2+诱导的 Aβ1-42聚集有显著抑制作用,并具有出良好的神经保护作用。可用于研究阿尔兹海默症。
产品描述
AChE-IN-12 is a potent and blood-brain barrier (BBB) penetrant acetylcholinesterase (AChE) with IC 50 s of 0.41 μM and 1.88 μM for rat AChE and electric eel AChE. AChE-IN-12 is also a good antioxidant (ORAC = 3.3 eq ), selective metal chelator and hu MAO-B inhibitor (IC 50 = 8.8 μM). AChE-IN-12 has remarkable inhibition of self- and Cu 2+ -induced Aβ 1-42 aggregation, as well as exhibits a good neuroprotective effect. AChE-IN-12 can be used for researching Alzheimer’s disease [1].
体外活性
AChE-IN-12 (compound 17f)(10-100 μM) exhibits no obvious cytotoxicity until the concentration increased up to 50 μM [1]. AChE-IN-12 (10 and 50 μM) adds up the cell viability of H 2 O 2 -induced PC12 cells [1]. Cell Cytotoxicity Assay Cell Line: PC12 cells [1] Concentration: 10, 50 and 100 μM Incubation Time: Result: Did not show obvious cytotoxicity until the concentration increased up to 50 μM. Cell Viability Assay Cell Line: PC12 cells (exposed to 100 μM H 2 O 2 for 1 hour to establish the oxidative damage model) [1] Concentration: 10 and 50 μM Incubation Time: Result: Added up the cell viability to 65.7% (p< 0.05) and 73.4% (p< 0.05) at 10 and 50 μM, respectively.
Cas No.
2764664-52-8
分子式
C33H41NO7
分子量
563.68
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years