A 844606
目录号 : GC15333
α7 nAChR partial agonist
Cas No.:861119-08-6
Sample solution is provided at 25 µL, 10mM.
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A 844606 is a potent and selective partial agonist of α7 nicotinic acetylcholine receptor (nAChR) with IC50 value of 11 nM [1].
The α7 nAChR is a nicotinic acetylcholine receptor and is located in the brain, spleen and lymphocytes of lymph nodes. The α7 nAChR plays an important role in the pathophysiology of neuropsychiatric diseases such as Alzheimer’s disease, schizophrenia, drug addiction and depression [2].
A 844606 is a potent and selective α7 nAChR partial agonist with IC50 values of 11 and >30000 nM for α7 and α4β2, respectively. In Xenopus oocytes expressed recombinant human and rat α7 nAChR, A 844606 showed agonist activity with EC50 values of 1.4 and 2.2 μM, respectively. In PC12 cells, A 844606 activated α7 nAChR, which stimulated ERK1/2 phosphorylation [1].
In the mouse brain, A 844606 showed high uptake. In monkey brain, A 844606 was mainly distributed in the thalamus and hippocampus and was low in the cerebellum. Also, A 844606 was reduced by pretreatment with SSR180711, an α7 nAChR agonist [2].
References:
[1]. Briggs CA, Schrimpf MR, Anderson DJ, et al. alpha7 nicotinic acetylcholine receptor agonist properties of tilorone and related tricyclic analogues. Br J Pharmacol, 2008, 153(5): 1054-1061.
[2]. Toyohara J, Ishiwata K, Sakata M, et al. In vivo evaluation of alpha7 nicotinic acetylcholine receptor agonists [11C]A-582941 and [11C]A-844606 in mice and conscious monkeys. PLoS One, 2010, 5(2): e8961.
| Cas No. | 861119-08-6 | SDF | |
| 化学名 | 2-((3aR,6aR)-5-methylhexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)-9H-xanthen-9-one | ||
| Canonical SMILES | O=C1C2=CC(N3C[C@@H](CN(C)C4)[C@H]4C3)=CC=C2OC5=CC=CC=C15 | ||
| 分子式 | C20H20N2O2 | 分子量 | 320.38 |
| 溶解度 | <1.6mg/ml in ethanol | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.1213 mL | 15.6065 mL | 31.2129 mL |
| 5 mM | 0.6243 mL | 3.1213 mL | 6.2426 mL |
| 10 mM | 0.3121 mL | 1.5606 mL | 3.1213 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet