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bis(7)-Tacrine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
bis(7)-Tacrine图片
CAS NO:224445-12-9
规格:98%
分子量:565.6
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
AChE inhibitor
CAS:224445-12-9
分子式:C33H40N4 ? 2HCl
分子量:565.6
纯度:98%
存储:Store at -20°C

Background:

IC50: 0.40 nM


bis(7)-Tacrine is an AChE inhibitor.


Acetylcholinesterase ( AChE), the primary cholinesterase in the body, is an enzyme catalyzing the breakdown of acetylcholine and of some other choline esters that function as neurotransmitters.


In vitro: bis(7)-Tacrine, the 9-amino-1,2,3,4-tetrahydroacridine (THA) dimer, was identified as a promising drug candidate for the palliative treatment of Alzheimer's disease, due to its significant enhancement in acetylcholinesterase (AChE) inhibition potency and AChE/butyrylcholinesterase (BChE) selectivity relative to THA itself. Enzyme kinetic studies performed in rat cortex found that both bis(7)-tacrine and THA exhibited mixed inhibition, and the rat cortex KI values were consistent with the previously determined human cerebellum Ki values [1].


In vivo: Previous study evaluated the neuropharmacological effects of THA on memory impairment caused by scopolamine injection. BALB/c mice were orally treated with THA at 10 mg/kg for 10 days. Results showed that THA significantly could reduce the total number of entry error and reference memory errors. In addition, THA also inhibited the AChE activity in the hippocampus significantly [2].


Clinical trial: So far, no clinical study has been conducted.


参考文献:
[1] Carlier, P. R.,Han, Y.F.,Chow, E.S.H., et al. Evaluation of short-tether Bis-THA AChE inhibitors. A further test of the dual binding site hypothesis. Bioorganic & Medicinal Chemistry 7, 351-357 (1999).
[2] Lee JS, Hong SS, Kim HG, Lee HW, Kim WY, Lee SK, Son CG.  Gongjin-Dan Enhances Hippocampal Memory in a Mouse Model of Scopolamine-Induced Amnesia. PLoS One. 2016 Aug 2;11(8):e0159823.