Ladostigil (Synonyms: TV-3326)

Cat. No.: HY-10399: Data Sheet Handling Instructions
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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

CAS No. : 209394-27-4

Size	Price	Stock
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution		Ask For Quote & Lead Time
Solution
10 mM * 1 mL in DMSO		Ask For Quote & Lead Time
Solid
5 mg		Ask For Quote & Lead Time
10 mg		Ask For Quote & Lead Time
25 mg		Ask For Quote & Lead Time
50 mg		Ask For Quote & Lead Time
100 mg		Ask For Quote & Lead Time

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

Other Forms of Ladostigil:

Ladostigil hydrochloride Get quote
Ladostigil hemitartrate Get quote

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•Related Small Molecules:

•Related Proteins:

View All Monoamine Oxidase Isoform Specific Products:

View All Isoforms

MAO-A MAO-B

View All Cholinesterase (ChE) Isoform Specific Products:

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.

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.

209394-27-4

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
10 mM	0.3672 mL	1.8359 mL	3.6719 mL

View the Complete Stock Solution Preparation Table

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 2.5 mg/mL (9.18 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

Handling Instructions (2659 KB)

References

[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

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

Ladostigil Related Classifications

Neurological Disease

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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