Tacrine hydrochloride hydrate

製品コードS3639 バッチS363901

印刷

化学情報

Chemical Structure Synonyms Tacrine, Tetrahydroaminacrine, Tetrahydroaminoacridine Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C13H14N2.xHCl.xH2O
分子量 198.26(free bases) CAS No. 206658-92-6
Solubility (25°C)* 体外 DMSO 50 mg/mL
Water 50 mg/mL
Ethanol 50 mg/mL
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HepG2 cells
濃度 300 μM
反応時間 5 h
実験の流れ

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.
動物実験 動物モデル Sprague-Dawley rats
投薬量 30 mg/kg
投与方法 p.o.

参考

  • https://pubmed.ncbi.nlm.nih.gov/25747977/
  • https://www.sciencedirect.com/science/article/pii/S1214021X14600892
  • https://pubmed.ncbi.nlm.nih.gov/1530666/

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。