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

Ladostigil (TV-3326) 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 exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease. Ladostigil 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 Chemical Structure

Ladostigil Chemical Structure

CAS No. : 209394-27-4

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Other Forms of Ladostigil:

Ladostigil Related Antibodies

Top Publications Citing Use of Products

View All Monoamine Oxidase Isoform Specific Products:

View All Isoforms
MAO-A MAO-B

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View All Isoforms
AChE BChE

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Ladostigil (TV-3326) 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 exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease[1][2]. Ladostigil 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 μM (IC50)

AChE

31.8 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
SK-N-SH IC50
1.05 mM
Compound: TV3326
Inhibition of apoptosis in human SK-N-SH cells assessed as increase in cleaved caspase-3 by Western blot analysis
Inhibition of apoptosis in human SK-N-SH cells assessed as increase in cleaved caspase-3 by Western blot analysis
[PMID: 30884327]
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[2].
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[2].

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

Ladostigil Related Antibodies
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[4].
Ladostigil (50 μmol/kg; single p.o.) 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

272.34

Formula

C16H20N2O2
CAS No.
SMILES

O=C(OC1=CC2=C(CC[C@H]2NCC#C)C=C1)N(CC)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (367.19 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 3.6719 mL 18.3594 mL 36.7188 mL
5 mM 0.7344 mL 3.6719 mL 7.3438 mL
View the Complete Stock Solution Preparation Table

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: 2.5 mg/mL (9.18 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (9.18 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.6719 mL 18.3594 mL 36.7188 mL 91.7970 mL
5 mM 0.7344 mL 3.6719 mL 7.3438 mL 18.3594 mL
10 mM 0.3672 mL 1.8359 mL 3.6719 mL 9.1797 mL
15 mM 0.2448 mL 1.2240 mL 2.4479 mL 6.1198 mL
20 mM 0.1836 mL 0.9180 mL 1.8359 mL 4.5899 mL
25 mM 0.1469 mL 0.7344 mL 1.4688 mL 3.6719 mL
30 mM 0.1224 mL 0.6120 mL 1.2240 mL 3.0599 mL
40 mM 0.0918 mL 0.4590 mL 0.9180 mL 2.2949 mL
50 mM 0.0734 mL 0.3672 mL 0.7344 mL 1.8359 mL
60 mM 0.0612 mL 0.3060 mL 0.6120 mL 1.5300 mL
80 mM 0.0459 mL 0.2295 mL 0.4590 mL 1.1475 mL
100 mM 0.0367 mL 0.1836 mL 0.3672 mL 0.9180 mL
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Ladostigil Related Classifications

Help & FAQs
  • 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.

Keywords:

Ladostigil209394-27-4TV-3326TV3326TV 3326Monoamine OxidaseCholinesterase (ChE)MAOmonoamineoxidaseacetylcholinesteraseAChEMAO-BdepressionAlzheimerInhibitorinhibitorinhibit

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