1. Neuronal Signaling
  2. Monoamine Oxidase Cholinesterase (ChE)
  3. Ladostigil hemitartrate

Ladostigil hemitartrate  (Synonyms: TV-3326 hemitartrate)

Cat. No.: HY-10400 Purity: 98.90%
COA Handling Instructions

Ladostigil (TV-3326) hemitartrate is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), 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.

For research use only. We do not sell to patients.

Ladostigil hemitartrate Chemical Structure

Ladostigil hemitartrate Chemical Structure

CAS No. : 209394-46-7

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 657 In-stock
Solution
10 mM * 1 mL in DMSO USD 657 In-stock
Solid
5 mg USD 430 In-stock
10 mg USD 690 In-stock
25 mg USD 1380 In-stock
50 mg   Get quote  
100 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Ladostigil (TV-3326) hemitartrate is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), 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[1][2]. 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.

IC50 & Target[1]

MAO-B

37.1 nM (IC50)

AChE

31.8 nM (IC50)

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].

MedChemExpress (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) 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

694.77

Formula

C16H20N2O2.1/2C4H6O6

CAS No.
Appearance

Solid

Color

White to off-white

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]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 60 mg/mL (86.36 mM; Need ultrasonic and warming)

DMSO : 50 mg/mL (71.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4393 mL 7.1966 mL 14.3933 mL
5 mM 0.2879 mL 1.4393 mL 2.8787 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (1.80 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.25 mg/mL (1.80 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 98.90%

References

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 1.4393 mL 7.1966 mL 14.3933 mL 35.9831 mL
5 mM 0.2879 mL 1.4393 mL 2.8787 mL 7.1966 mL
10 mM 0.1439 mL 0.7197 mL 1.4393 mL 3.5983 mL
15 mM 0.0960 mL 0.4798 mL 0.9596 mL 2.3989 mL
20 mM 0.0720 mL 0.3598 mL 0.7197 mL 1.7992 mL
25 mM 0.0576 mL 0.2879 mL 0.5757 mL 1.4393 mL
30 mM 0.0480 mL 0.2399 mL 0.4798 mL 1.1994 mL
40 mM 0.0360 mL 0.1799 mL 0.3598 mL 0.8996 mL
50 mM 0.0288 mL 0.1439 mL 0.2879 mL 0.7197 mL
60 mM 0.0240 mL 0.1199 mL 0.2399 mL 0.5997 mL
H2O 80 mM 0.0180 mL 0.0900 mL 0.1799 mL 0.4498 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.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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