Tacrine hydrochloride hydrate

Catalog No.S3639 Batch:S363901

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Technical Data

Formula

C13H14N2.xHCl.xH2O
Molecular Weight 198.26(free bases) CAS No. 206658-92-6
Solubility (25°C)* In vitro DMSO 50 mg/mL
Water 50 mg/mL
Ethanol 50 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 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.
Targets
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].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    HepG2 cells

  • Concentrations

    300 μM

  • Incubation Time

    5 h

  • Method

    The level of H2O2 generation was monitored in HepG2 cells by adding the DCFH-DA. After treatment of 10–100 µM LQ for 12 h prior to the addition of 300 µM tacrine for 5h, cells were stained with 50 µM DCFH-DA for 1 h. DCFH oxidation was determined at excitation and emission wavelengths of 485 and 530 nm using a microplate reader.
Animal Study:

[1]
  • Animal Models

    Sprague-Dawley rats

  • Dosages

    30 mg/kg

  • Administration

    p.o.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.