Dual AChE-MAO B-IN-3 (compound C10) 是一种有效的双AChE/MAO-B抑制剂,IC50值分别为 0.58 和 0.41 μM。Dual AChE-MAO B-IN-3 是一种双结合抑制剂,能与 AChE 的催化阴离子位点和外周阴离子位点结合。Dual AChE-MAO B-IN-3 可以用于阿尔茨海默病 (AD) 的研究。
生物活性 | Dual AChE-MAO B-IN-3 (compound C10) is a potent dualAChE/MAO-Binhibitior, withIC50values of 0.58 and 0.41 μM, respectively. Dual AChE-MAO B-IN-3 is a dual-binding inhibitor bound to both the catalytic anionic site and peripheral anionic site ofAChE. Dual AChE-MAO B-IN-3 can be used for Alzheimer’s disease (AD) research[1]. |
IC50& Target | MAO-B 0.41 ± 0.0 μM (IC50) | EeAChE 0.58 ± 0.0 μM (IC50) |
|
体外研究 (In Vitro) | Dual AChE-MAO B-IN-3 (compound C10) (0-100 μM, 24 h) exhibits low neurotoxicity, and (0-10 μM, 24 h) potently inhibits AChE enzymatic activity[1]. Dual AChE-MAO B-IN-3 more effectively protects against mitochondrial dysfunction and oxidation thanDonepezil(HY-14566), strongly inhibits AChE-induced amyloid aggregation, and moderately reduces glutaraldehyde-induced phosphorylation of tau protein in SH-SY5Y cells[1].
Cell Viability Assay[1] Cell Line: | SH-SY5Y cells | Concentration: | 10 μM, 50 μM, 100 μM | Incubation Time: | 24 h | Result: | Exhibited a nonsignificant reduction in cell viabilities up to the maximum tested concentration of 100 μM. The percentage cell viability at 10-100 μM was observed in the range of 96.92–99.58%. Showed that compound C10 was not toxic to SH-SY5Y neuroblastoma cells at concentrations up to 100 μM. |
|
体内研究 (In Vivo) | Dual AChE-MAO B-IN-3 (compound C10) (10 mg/kg, IP, once daily for 10 consecutive days) displays largely enhanced improvements in cognitive behaviors and spatial memory in a scopolamine-induced AD mice model with better efficacy thanDonepezil(HY-14566)[1].
Animal Model: | ICR mice (female, 8-10 weeks, 25-30 g)[1] | Dosage: | 10 mg/kg | Administration: | IP, once daily for 10 consecutive days | Result: | Significantly ameliorated the cognitive impairment in a scopolamine-induced mice model. |
|
分子量 | |
Formula | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |