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产品总数：60947
| 中文名称 |
Ladostigil hemitartrate
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|---|---|
| 中文别名 |
乙基甲基-氨基甲酸 (3R)-2,3-二氢-3-(2-丙炔氨基)-1H-茚-5-基酯酒石酸盐
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| 英文名称 |
Ladostigil hemitartrate
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| 英文别名 |
Ladostigil tartrate;Ethylmethyl-carbamic acid (3R)-2,3-dihydro-3-(2-propynylamino)-1H-inden-5-yl ester (2R,3R)-2,3-dihydroxybutanedioate (2:1);(2R,3R)-2,3-dihydroxybutanedioic acid,[(3R)-3-(prop-2-ynylamino)-2,3-dihydro-1H-inden-5-yl] N-ethyl-N-methylcarbamate;(3R)-3-(prop-2-ynylamino)-2,3,-dihydro-1H-indan-5-yl ethyl methyl carbamate tartrate;ethylmethylcarbamic acid (3R)-2,3-dihydro-3-(2-propynylamino)-1H-inden-5-yl ester (2R,3R)-2,3-dihydroxybutanedioate;R(+)-6-(N-methyl-N-ethylcarbamoyloxy)-N'-propargyl-1-aminoindan L-tartrate;R(+)-6-(N-methyl-N-ethylcarbamoyloxy)-N'-propargyl-1-aminoindan tartrate;TV-3219;UNII-2J1346C51H;Ladostigil hemitartrate
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| Cas No. |
209394-46-7
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| 分子式 |
C16H20N2O2.C4H6O6
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| 分子量 |
422.43
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| 包装储存 |
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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| 产品详情 |
Ladostigil (TV-3326) hemitartrate 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 hemitartrate 具有神经保护，抗氧化和抗炎作用，可用于抑郁症和阿尔茨海默症的研究。
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| 生物活性 |
Ladostigil (TV-3326) hemitartrate 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 hemitartrate exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil hemitartrate can be used for the research of depression and Alzheimers disease.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
MAO-B 37.1 nM (IC50) AChE 31.8 nM (IC
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| 体外研究(In Vitro) |
Ladostigil (1-10 μM) hemitartrate 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) hemitartrate 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.
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| 体内研究(In Vivo) |
Ladostigil (17 mg/kg; p.o. daily for 6 weeks) hemitartrate 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.) hemitartrate 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.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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| ClinicalTrial |
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| 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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| 溶解度数据 |
In Vitro: H2O : 100 mg/mL (143.93 mM; Need ultrasonic)DMSO : 50 mg/mL (71.97 mM; Need ultrasonic)配制储备液
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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。
2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。
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