| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
MAO-B 37.1 μM (IC50) AChE 31.8 μM (IC50)
Ladostigil targets both cholinesterase (AChE) and brain-selective monoamine oxidase (MAO-B). By inhibiting these enzymes, it increases the levels of acetylcholine and monoamine neurotransmitters like dopamine in the brain. This dual mechanism is designed to provide symptomatic relief and potentially modify the course of neurodegenerative diseases. |
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| ln Vitro |
Neuroprotective effects of ladostigil (1–10 µM) include halting the decline of the mitochondrial membrane potential (ψ), reducing the intensity of apoptotic cascades, and preventing the generation of reactive oxygen species (ROS) brought on by OS insults[2]. Significant neuroprotective effects of lastigil (1–10 µM) on human neuroblastoma SK-N-SH cells include reduction of Bad and Bax gene and protein expression, increase of Bcl-2, and inhibition of caspase-3 activation[2].
In vitro, Ladostigil acts as a dual inhibitor, with reported IC50 values of 37.1 μM for MAO-B and 31.8 μM for AChE. Its activity is typically measured using standard enzymatic assays for each target. The compound's antioxidant and anti-inflammatory properties are also evaluated in cell-based models of neuroinflammation and oxidative stress. |
| ln Vivo |
In the forced swim tests (FST) and elevated plus maze (EPM) tests, ladostigil (17 mg/kg; po daily for 6 weeks) completely eliminates their depressive-like behavior and hyperanxiety in adulthood, from puberty to prenatally stressed rats[4]. In the object recognition test, rats given 50 μmol/kg of latstigil as a single dose recover their lost episodic memory[3].
In vivo, Ladostigil has demonstrated neuroprotective effects in preclinical models. As an orally active compound, it can be administered to animals to study its effects on cognitive function, neuroinflammation, and neurodegeneration. It has been investigated in a clinical trial (NCT01429623) for patients with mild cognitive impairment, indicating its translational potential. |
| Enzyme Assay |
Non-cell-based assays for Ladostigil involve incubating the compound with MAO-B or AChE enzymes. For AChE, the Ellman's method using acetylthiocholine as a substrate is standard. For MAO-B, a fluorometric assay with a specific substrate is used. The inhibition of enzyme activity is measured, and IC50 values (e.g., 37.1 μM for MAO-B and 31.8 μM for AChE) are calculated from the inhibition curves.
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| Cell Assay |
For in vitro cellular assays, Ladostigil can be tested on neuronal cell lines to assess its neuroprotective effects. Cells are pre-treated with the compound and then exposed to neurotoxic agents or inflammatory stimuli. Outcomes such as cell viability, levels of oxidative stress markers, and inflammatory cytokine production are measured to evaluate its protective and anti-inflammatory properties.
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| Animal Protocol |
Animal/Disease Models: Pathogen-free (SPF) SD (Sprague-Dawley) rats[4]
Doses: 17 mg/kg Route of Administration: Po (added to the drinking water) daily for 6 weeks Experimental Results: Inhibited brain MAO-A and B by more than 60%. decreased hyperanxiety of male and female prenatally stressed (PS) rats in the EPM and depressive-like behavior in the FST. In vivo animal studies for Ladostigil typically involve oral administration to rodents. Its efficacy can be assessed in models of Alzheimer's disease (e.g., transgenic mice) or depression, where cognitive function, behavioral outcomes, and neurochemical changes are measured. The compound's ability to inhibit brain AChE and MAO-B activity is confirmed ex vivo. |
| ADME/Pharmacokinetics |
Ladostigil has a molecular weight of 272.34 g/mol and a molecular formula of C16H20N2O2. It is an orally active compound. The free base is also known as TV-3326. It is a research compound and should be stored according to the manufacturer's instructions, typically as a powder at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
The toxicity profile of Ladostigil is not fully detailed in the provided search results. As a research compound that has entered clinical trials, its safety has been evaluated to some extent. Common side effects may be related to its cholinesterase inhibitory activity. It is intended for research use only and should be handled with standard laboratory safety practices.
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| References |
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| Additional Infomation |
Ladostigil belongs to the indane class of drugs. Ladostigil is currently being investigated in the clinical trial NCT01429623 (a 3-year study designed to evaluate the safety and efficacy of low-dose Ladostigil in patients with mild cognitive impairment).
Ladostigil (CAS#: 209394-27-4) is a novel, orally active, dual inhibitor of MAO-B and AChE. Its multi-target mechanism, which combines cholinesterase inhibition with brain-selective MAO inhibition and antioxidant properties, makes it a promising candidate for the treatment of neurodegenerative disorders. It is currently being researched for Alzheimer's disease and depression. |
| Molecular Formula |
C16H20N2O2
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|---|---|
| Molecular Weight |
272.34
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| Exact Mass |
272.152
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| CAS # |
209394-27-4
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| Related CAS # |
Ladostigil hydrochloride;209394-18-3;Ladostigil hemitartrate;209394-46-7
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| PubChem CID |
208907
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| Appearance |
Typically exists as solid at room temperature
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| Vapour Pressure |
5.19E-07mmHg at 25°C
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| LogP |
2.738
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
20
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| Complexity |
387
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C#CCN[C@@H]1CCC2=C1C=C(C=C2)OC(=O)N(C)CC
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| InChi Key |
LHXOCOHMBFOVJS-OAHLLOKOSA-N
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| InChi Code |
InChI=1S/C16H20N2O2/c1-4-10-17-15-9-7-12-6-8-13(11-14(12)15)20-16(19)18(3)5-2/h1,6,8,11,15,17H,5,7,9-10H2,2-3H3/t15-/m1/s1
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| Chemical Name |
[(3R)-3-(prop-2-ynylamino)-2,3-dihydro-1H-inden-5-yl] N-ethyl-N-methylcarbamate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~367.2 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (9.18 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (9.18 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: 2.5 mg/mL (9.18 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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