CAS NO: | 224445-12-9 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Cas No. | 224445-12-9 |
别名 | 1,7-N-heptylene-bis-9,9'-amino-1,2,3,4-tetrahydro-acridine |
化学名 | 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 |
分子式 | C33H40N4o 2HCl |
分子量 | 565.6 |
溶解度 | ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide |
储存条件 | Store at -20℃ |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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: |