Home Neuronal Signaling AChR inhibitor - HNMT inhibitor Tacrine hydrochloride hydrate

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Tacrine hydrochloride hydrate AChR inhibitor

Cat.No.S3639

Tacrine (Tetrahydroaminacrine, Tetrahydroaminoacridine) is a centerally active cholinesterase inhibitor that has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders. It also acts as a histamine N-methyltransferase inhibitor.
Tacrine hydrochloride hydrate AChR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 198.26(free bases)

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Quality Control

Chemical Information, Storage & Stability

Molecular Weight 198.26(free bases) Formula

C13H14N2.xHCl.xH2O

 Storage (From the date of receipt)
CAS No. 206658-92-6 Download SDF Storage of Stock Solutions

Synonyms Tacrine, Tetrahydroaminacrine, Tetrahydroaminoacridine Smiles C1CCC2=NC3=CC=CC=C3C(=C2C1)N.O.Cl

Solubility

In vitro
Batch:

DMSO : 50 mg/mL ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 50 mg/mL

Ethanol : 50 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
HNMT [3]
cholinesterase [1]
In vitro
Tacirne is an active cholinesterase inhibitor that blocks the degradation of cholinergic nerves in the cerebral cortex and hippocampus to increase cholinergic transmission. Tacrine induces hepatic damages in vitro. It can also induce oxidative stress and mitochondrial dysfunction. Tacrine treatment in HepG2 cells markedly inhibits the phosphorylation of GSK3β[1].
In vivo
In rats, tacrine increased markers of liver damages (ALT and AST), degenerative region areas, and numbers of infiltrating inflammatory cells. Tacrine is known to induce hepatocyte necrosis and degeneration[1]. In the past, tacrine was used for the treatment of cognitive dysfunction during vascular dementia and Alzheimer disease. It is found to abolish lipopolysaccharide induced inflammation including IL-6 secretion in the central nervous system. Tacrine can aggravate the progress of tularemia in a mouse model--the effect would be beneficial in several pathologies such as neurodegenerative disorders; e.g. the positive effect of tacrine when used in therapy for Alzheimer's disease would be attributed to its anti-inflammatory action in addition to any improvement in cognitive functions[2].
References

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