Ladostigil

CAS: 209394-27-4 货号: L649674 分子式: C16H20N2O2 分子量: 272.34 PubChem CID: 208907
有货
别名
拉多斯蒂吉尔
储存条件
-20°C储存
运输条件
超低温运输
★
规格
库存
价格
数量
5mg
L649674-5mg
期货 Stock Image
¥4,500.90
10mg
L649674-10mg
期货 Stock Image
¥8,000.90
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。

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质量文档

SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


Ladostigil (TV-3326) is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO) , with IC 50 s of 37.1 and 31.8 μM for MAO-B and AChE , respectively. Ladostigil exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease

In Vitro

Ladostigil (1-10 µM) exerts neuroprotective activities, including a prevention of the fall of the mitochondrial membrane potential (ψ), attenuation of apoptotic cascades and an inhibition of ROS production induced by OS insults. Ladostigil (1-10 µM) has a significant neuroprotective activity, including inhibition of caspase-3 activation, induction of Bcl-2 and reduction of Bad and Bax gene and protein expression in human neuroblastoma SK-N-SH cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Ladostigil (17 mg/kg; p.o. daily for 6 weeks) abolishes their hyperanxiety and depressive-like behaviour in the elevated plus maze (EPM) and forced swim tests (FST) tests in adulthood from puberty to prenatally-stressed rats. Ladostigil (50 μmol/kg; single p.o.) restores the loss of episodic memory in the object recognition test in rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Pathogen-free (SPF) Sprague-Dawley ratsDosage: 17 mg/kg Administration: P.o. (added to the drinking water) daily for 6 weeks Result: Inhibited brain MAO-A and B by more than 60%. Reduced hyperanxiety of male and female prenatally stressed (PS) rats in the EPM and depressive-like behaviour in the FST.

IC50& Target:MAO-B 37.1 μM (IC 50 ) AChE 31.8 μM (IC 50 )

规格

别名
拉多斯蒂吉尔
英文名称
Ladostigil
生化机理
Ladostigil(TV-3326)是一种口服活性胆碱酯酶和脑选择性单胺氧化酶(MAO)双重抑制剂,对 MAO-B 和 AChE 的 IC 50 s 分别为 37.1 μM 和 31.8 μM。拉多斯替吉具有神经保护、抗氧化和抗炎作用。
储存条件
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CCN(C)C(=O)OC1=CC2=C(CC[C@H]2NCC#C)C=C1
PubChem CID
分子量
272.34

技术文档

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🔬 规格说明书

该级别的完整质量属性和验收标准。

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高级数据

关联靶点(人)
MAOA Tclin Monoamine oxidase A (11911 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ACHE Tclin Acetylcholinesterase (18204 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAOB Tclin Monoamine oxidase B (8835 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
BCHE Tclin Butyrylcholinesterase (7174 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SK-N-SH (1499 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
关联靶点(其它种属)
Oryctolagus cuniculus (11301 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mus musculus (284745 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
H9c2 (3506 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
BCHE Cholinesterase (8742 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
作用机制
作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献
化学和物理性质
分子量
272.340 g/mol
XLogP3
2.000
氢键供体数Hydrogen Bond Donor Count
1
氢键受体数Hydrogen Bond Acceptor Count
3
可旋转键计数Rotatable Bond Count
5
精确质量Exact Mass
272.152 Da
单同位素质量Monoisotopic Mass
272.152 Da
拓扑极表面积Topological Polar Surface Area
41.600 Ų
重原子数Heavy Atom Count
20
形式电荷Formal Charge
0
复杂度Complexity
387.000
同位素原子数Isotope Atom Count
0
定义的原子立体中心计数Defined Atom Stereocenter Count
1
未定义的原子立体中心计数Undefined Atom Stereocenter Count
0
定义的键立体中心计数Defined Bond Stereocenter Count
0
未定义的键立体中心计数Undefined Bond Stereocenter Count
0
所有立体化学键的总数The total count of all stereochemical bonds
0
共价键合单元计数Covalently-Bonded Unit Count
1
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