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。
生物活性 | Ladostigil (TV-3326) hemitartrate is an orally active dual inhibitor ofcholinesteraseand brain-selectivemonoamine oxidase(MAO), withIC50s of 37.1 and 31.8 μM forMAO-BandAChE, respectively. Ladostigil hemitartrate exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil hemitartrate can be used for the research of depression and Alzheimer's disease[1][2]. |
IC50& Target[1] | MAO-B 37.1 nM (IC50) | AChE 31.8 nM (IC50) |
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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[2]. 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[2].
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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[4]. Ladostigil (50 μmol/kg; single p.o.) hemitartrate restores the loss of episodic memory in the object recognition test in rats[3].
Animal Model: | Pathogen-free (SPF) Sprague-Dawley rats[4] | Dosage: | 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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | 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 1 mM | 1.4393 mL | 7.1966 mL | 14.3933 mL | 5 mM | 0.2879 mL | 1.4393 mL | 2.8787 mL | 10 mM | 0.1439 mL | 0.7197 mL | 1.4393 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 1.25 mg/mL (1.80 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (1.80 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 1.25 mg/mL (1.80 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (1.80 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 1.25 mg/mL (1.80 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (1.80 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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