Ladostigil|209394-27-4|(TV-3326)-陌孚医药/Medlife

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Ladostigil (Synonyms: TV-3326)

目录号: PL07498

CAS No. :209394-27-4

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中文名称	Ladostigil
英文名称	Ladostigil
英文别名	Ladostigil;(3R)-3-(Prop-2-ynylamino)indan-5-yl ethyl(methyl)carbamate;carbamic acid, N-ethyl-N-methyl-, (3R)-2,3-dihydro-3-(2-propyn-1-ylamino)-1H-inden-5-yl ester
Cas No.	209394-27-4
分子式	C₁₆H₂₀N₂O₂
分子量	272.34
包装储存	Please store the product under the recommended conditions in the Certificate of Analysis.

产品详情

Ladostigil (TV-3326) 是一种口服有效的胆碱酯酶 (cholinesterase) 和脑选择性单胺氧化酶 (MAO) 的双重抑制剂，抑制 MAO-B 和 AChE 的 IC₅₀ 值分别为 37.1 和 31.8 μM。Ladostigil 具有神经保护，抗氧化和抗炎的作用，可用于抑郁症和阿尔茨海默症的研究。

生物活性

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 Alzheimers disease.

IC50 & Target[1][2]

MAO-B 37.1 μM (IC50) AChE 31.8 μM (IC

体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

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.

ClinicalTrial

参考文献

[1]. Denya I, et, al. Design, synthesis and evaluation of indole derivatives as multifunctional agents against Alzheimers disease. Medchemcomm. 2018 Jan 16; 9(2):357-370.
[2]. Weinreb O, et, al. Ladostigil: a novel multimodal neuroprotective drug with cholinesterase and brain-selective monoamine oxidase inhibitory activities for Alzheimers disease treatment. Curr Drug Targets. 2012 Apr; 13(4): 483-94.

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