bis(7)-Tacrine
(Synonyms: 1,7-N-heptylene-bis-9,9'-amino-1,2,3,4-tetrahydro-acridine) 目录号 : GC15628
A potent acetylcholinesterase inhibitor
Cas No.:224445-12-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
| Cas No. | 224445-12-9 | SDF | |
| 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 | C33H40N4 • 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°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.768 mL | 8.8402 mL | 17.6803 mL |
| 5 mM | 0.3536 mL | 1.768 mL | 3.5361 mL |
| 10 mM | 0.1768 mL | 0.884 mL | 1.768 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。