| CAS NO: | 224445-12-9 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 565.6 |
| Cas No. | 224445-12-9 |
| Formula | C33H40N4·2HCl |
| Synonyms | 1,7-N-heptylene-bis-9,9'-amino-1,2,3,4-tetrahydro-acridine |
| Solubility | ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide |
| Chemical Name | N,N'-bis(1,2,3,4-tetrahydro-9-acridinyl)-1,7-heptanediamine, dihydrochloride |
| Canonical SMILES | [H]N(CCCCCCCN([H])C1=C(C=CC=C2)C2=NC3=C1CCCC3)C4=C5C(C=CC=C5)=NC6=C4CCCC6.Cl.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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.
References:
[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.
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