Tacrine HCl

製品コードS4357 バッチS435701

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C13H14N2.HCl

分子量 234.72 CAS No. 1684-40-8
Solubility (25°C)* 体外 DMSO 46 mg/mL (195.97 mM)
Water 46 mg/mL (195.97 mM)
Ethanol 46 mg/mL (195.97 mM)
* <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 is a centrally acting anticholinesterase and indirect cholinergic agonist. Tacrine hydrochloride hydrate is an inhibitor of both acetyl (AChE) and butyryl-cholinestrase (BChE) with IC50s of 31 nM and 25.6 nM, respectively.
in vitro

Tacrine hydrochloride is an inhibitor of three different hepatic microsomal cytochrome P-450 enzyme sub-families. Tacrine hydrochloride at 40 mg/mL, 80 mg/mL or 200 mg/mL inhibits 3-hydroxymethyl antipyrine (HMA) production by 17%, 24% and 41% and OHA production by 52%, 55% and 79%, respectively, in hepatic microsome. [1] Tacrine severely inhibits normal levels of secretion of soluble APP derivatives by cells into conditioned media in glial, fibroblast, pheochromocytoma (PC12), and neuroblastoma cells. Tacrine treatment does not alter the level of HSP-70 in cell extracts and tacrine affected mildly the secretion of PN-1 in neuroblastoma and PC12 cells. [2] Tacrine (1 μM) attenuates the neurotoxic effect of A beta(25-35) in rat PC12 cells. [3]

in vivo

Tacrine (3 mg/kg, i.p.) prevents the avoidance impairment induced by 5 mg/kg amitriptyline on shuttle-box avoidance acquisition as well as on a previously learned avoidance response in mice. [4] Tacrine (5mg/kg) shows significant effects of the inhibition of brain AChE for more than 6 hours in the rat hippocampus. Tacrine (5mg/kg) increases acetylcholine concentration in the synaptic cleft of the hippocampus mostly through AChE inhibition in the rat hippocampus, and the maximum increases are observed at about 1.5 hours. [5]

プロトコル(参考用のみ)

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。