Dual AChE-MAO B-IN-3

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

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

505.53

Formula

C₃₀H₂₆F₃NO₃

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.