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Ladostigil

Catalog No. T32535   CAS 209394-27-4
Synonyms: TV-3326, Ladostigil, TV 3326, TV3326, Ladostigil free base

Ladostigil (Ladostigil free base) is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO) with inhibitory effects on MAO-B and AChE, with IC50 values of 37.1 and 31.8 μM, respectively.Ladostigil possesses anti-inflammatory, antioxidant, and neuroprotective activities, and may be used in studies of depression and Alzheimer's disease.

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Ladostigil Chemical Structure
Ladostigil, CAS 209394-27-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 120.00
5 mg In stock $ 290.00
10 mg In stock $ 440.00
25 mg In stock $ 728.00
50 mg In stock $ 987.00
100 mg In stock $ 1,390.00
500 mg In stock $ 2,770.00
1 mL * 10 mM (in DMSO) In stock $ 277.00
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Purity: 98.79%
ee: 98.58%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Ladostigil (Ladostigil free base) is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO) with inhibitory effects on MAO-B and AChE, with IC50 values of 37.1 and 31.8 μM, respectively.Ladostigil possesses anti-inflammatory, antioxidant, and neuroprotective activities, and may be used in studies of depression and Alzheimer's disease.
Targets&IC50 AChE:31.8 μM, MAO-B:37.1 μM
In vitro Ladostigil (1-10 µM) demonstrates neuroprotective effects by preventing the decline in mitochondrial membrane potential (ψ), reducing apoptotic cascades, and inhibiting the production of reactive oxygen species (ROS) induced by OS insults.[6] Ladostigil (1-10 µM) exhibits notable neuroprotective effects in human neuroblastoma SK-N-SH cells. These effects involve the inhibition of caspase-3 activation, upregulation of Bcl-2 expression, and downregulation of Bad and Bax gene and protein expression.[6]
In vivo Ladostigil (17 mg/kg; p.o. daily for 6 weeks) eliminates hyperanxiety and depressive-like behavior in adulthood in rats exposed to prenatal stress, spanning from puberty to the adult stage. This effect is demonstrated in both the elevated plus maze (EPM) and forced swim tests (FST).[8] Ladostigil (50 μmol/kg; single p.o.) restores the loss of episodic memory in the object recognition test in rats.[7]
Synonyms TV-3326, Ladostigil, TV 3326, TV3326, Ladostigil free base
Molecular Weight 272.34
Formula C16H20N2O2
CAS No. 209394-27-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4.8 mg/mL (17.63 mM)

TargetMolReferences and Literature

1. Bar-Am O, et al. Neuroprotective and neurorestorative potential of propargylamine derivatives in ageing: focus on mitochondrial targets. J Neural Transm (Vienna). 2016 Feb;123(2):125-135. 2. Moradov D, et al. Dose-limiting inhibition of acetylcholinesterase by ladostigil results from the rapid formation and fast hydrolysis of the drug-enzyme complex formed by its major metabolite, R-MCPAI. Biochem Pharmacol. 2015;94(2):164-172. 3. Goelman G, et al. Functional connectivity in prenatally stressed rats with and without maternal treatment with ladostigil, a brain-selective monoamine oxidase inhibitor. Eur J Neurosci. 2014;40(5):2734-274 4. Bansal Y, et al. Multifunctional compounds: smart molecules for multifactorial diseases. Eur J Med Chem. 2014;76:31-42. 5. Denya I, et al. Design, synthesis and evaluation of indole derivatives as multifunctional agents against Alzheimer's disease. Medchemcomm. 2018;9(2):357-370. 6. 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;13(4):483-494. 7. Weinstock M, et al. Ladostigil, a novel multifunctional drug for the treatment of dementia co-morbid with depression. J Neural Transm Suppl. 2006;(70):443-446. 8. 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;181(1):118-125.

Related compound libraries

This product is contained In the following compound libraries:
Clinical Compound Library Bioactive Compound Library Bioactive Compounds Library Max Neuronal Signaling Compound Library

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Keywords

Ladostigil 209394-27-4 Metabolism Neuroscience oxidation-reduction Antioxidant MAO AChE TV-3326 TV 3326 TV3326 Ladostigil free base inhibitor inhibit

 

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