Ladostigil hemitartrate
Based on 1 Customer Validation
Ladostigil (TV-3326) hemitartrate is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO) that can cross the blood-brain barrier, with IC50s 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 Alzheimer's disease. Ladostigil (hemitartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- Pureza: 98.90%
- No. CAS: 209394-46-7
- Fòrmula: C16H20N2O2·1/2C4H6O6
- Peso molecular:347.40
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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MAO-B 37.1 nM (IC50) |
AChE 31.8 nM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ladostigil (50 μmol/kg; single p.o.) hemitartrate restores the loss of episodic memory in the object recognition test in rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Pathogen-free (SPF) Sprague-Dawley rats[4]
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Dosage:17 mg/kg
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Administration:P.o. (added to the drinking water) daily for 6 weeks
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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.
Chemical Information
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No. CAS 209394-46-7
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Appearance Solid
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Peso molecular 347.40
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Fòrmula C16H20N2O2·1/2C4H6O6
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Color White to off-white
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SMILES
O=C(OC1=CC2=C(CC[C@H]2NCC#C)C=C1)N(CC)C.OC([C@H](O)[C@@H](O)C(O)=O)=O.[1/2]
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Synonyms
TV-3326 hemitartrate
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
H2O : 60 mg/mL (172.71 mM; Need ultrasonic and warming)
DMSO : 50 mg/mL (143.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (3.60 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (3.60 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (584 KB)
- English - EN (584 KB)
- Français - FR (584 KB)
- Deutsch - DE (584 KB)
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- Italian - IT (584 KB)
- Korean - KR (584 KB)
- Portuguese - PT (584 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Denya I, et, al. Design, synthesis and evaluation of indole derivatives as multifunctional agents against Alzheimer's disease. Medchemcomm. 2018 Jan 16;9(2):357-370. [Content Brief]
[2]. Weinreb O, et, al. Ladostigil: a novel multimodal neuroprotective drug with cholinesterase and brain-selective monoamine oxidase inhibitory activities for Alzheimer's disease treatment. Curr Drug Targets. 2012 Apr;13(4):483-94. [Content Brief]
[3]. Weinstock M, et, al. Ladostigil, a novel multifunctional drug for the treatment of dementia co-morbid with depression. J Neural Transm Suppl. 2006;(70):443-6. [Content Brief]
[4]. Poltyrev T, et, al. Effect of chronic treatment with ladostigil (TV-3326) on anxiogenic and depressive-like behaviour and on activity of the hypothalamic-pituitary-adrenal axis in male and female prenatally stressed rats. Psychopharmacology (Berl). 2005 Aug;181(1):118-25. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.8785 mL | 14.3926 mL | 28.7853 mL | 71.9632 mL |
| 5 mM | 0.5757 mL | 2.8785 mL | 5.7571 mL | 14.3926 mL | |
| 10 mM | 0.2879 mL | 1.4393 mL | 2.8785 mL | 7.1963 mL | |
| 15 mM | 0.1919 mL | 0.9595 mL | 1.9190 mL | 4.7975 mL | |
| 20 mM | 0.1439 mL | 0.7196 mL | 1.4393 mL | 3.5982 mL | |
| 25 mM | 0.1151 mL | 0.5757 mL | 1.1514 mL | 2.8785 mL | |
| 30 mM | 0.0960 mL | 0.4798 mL | 0.9595 mL | 2.3988 mL | |
| 40 mM | 0.0720 mL | 0.3598 mL | 0.7196 mL | 1.7991 mL | |
| 50 mM | 0.0576 mL | 0.2879 mL | 0.5757 mL | 1.4393 mL | |
| 60 mM | 0.0480 mL | 0.2399 mL | 0.4798 mL | 1.1994 mL | |
| 80 mM | 0.0360 mL | 0.1799 mL | 0.3598 mL | 0.8995 mL | |
| 100 mM | 0.0288 mL | 0.1439 mL | 0.2879 mL | 0.7196 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Ladostigil hemitartrate Related Classifications
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