1. Neuronal Signaling
  2. Monoamine Oxidase Cholinesterase (ChE)
  3. MAO-A/B-IN-3

MAO-A/B-IN-3 (Compound 12) 是一种双重 MAO-AChE 抑制剂,对 MAO-AMAO-BAChE 均展现出优越的多靶点活性,IC50 值分别为 67 nM、29 nM 和 1370 nM。MAO-A/B-IN-3 可修饰甲酮胺类 MTDL 中的 A 位 (疏水环) 和 C 位 (半羰基肼链) 以此增强 MAO-A/B 的抑制潜力,并显著降低 AChE的抑制活性。MAO-A/B-IN-3 有望用于神经退行性疾病领域研究。

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MAO-A/B-IN-3 Chemical Structure

MAO-A/B-IN-3 Chemical Structure

CAS No. : 315210-31-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MAO-A/B-IN-3 (Compound 12) stands out as a key dual MAO-AChE inhibitor, displaying excellent multi-target efficacy against MAO-A, MAO-B, and AChE with IC50 values of 67 nM, 29 nM, and 1370 nM respectively. MAO-A/B-IN-3 is adept at altering the A site (hydrophobic ring) and C site (semicarbazone chain) within ketone amine-based MTDLs to bolster the inhibitory potential against MAO-A/B while notably diminishing activity against AChE. MAO-A/B-IN-3 is poised for research applications in the field of neurodegenerative diseases[1].

IC50 & Target[1]

MAO-A

67 nM (IC50)

MAO-B

29 nM (IC50)

AChE

1370 nM (IC50)

体外研究
(In Vitro)

MAO-A/B-IN-3 (Compound 12) 在体外Caco2细胞穿透性实验中表现出中等的渗透性 (16.49 nm/s) [1]
MAO-A/B-IN-3 对MDCK细胞显示出中等的穿透性 (103.16 nm/s) [1]
MAO-A/B-IN-3 显示90.97%的血浆蛋白结合率,结合率大于90% 代表强结合率,表明它具有较长的半衰期和缓慢的排泄特性[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

MAO-A/B-IN-3 (Compound 12) (20 mg/kg;腹腔注射;60分钟) 增加了动物的不动期,因此被认为是中枢神经系统抑制剂[1]
MAO-A/B-IN-3 (30 mg/kg;腹腔注射;30分钟) 具有显著的抗焦虑活性,其中一些化合物显示出比参考药物地西泮更优越的活性[1]
MAO-A/B-IN-3 (30 mg/kg;腹腔注射;0.5小时和4小时) 在雄性白种小鼠中至少到4小时内不具有神经毒性[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

308.33

Formula

C17H16N4O2

CAS 号
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.

纯度 & 产品资料
参考文献
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产品名称:
MAO-A/B-IN-3
目录号:
HY-162606
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