Astemizole
(Synonyms: 阿司咪唑; R 43512) 目录号 : GC16945
A histamine H1 receptor antagonist and ERG channel blocker
Cas No.:68844-77-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Astemizole is a potent anti-histamine compound that antagonizes the histamine H1-receptor with IC50 of 4 nM. It is also identified less potent at muscarinic acetylcholine receptors with Ki of 2.4 µM.
The histamine H1 receptor, a member of Rhodopsin-like G-protein-coupled receptors, is activated by the biogenic amine histamine and is expressed throughout the body, particularly in smooth muscles, on vascular endothelial cells, in the central nervous system, and in the heart.
Astemizole targets imperative proteins included in tumor movement, to be specific, either à-go-go 1 (Eag1) and Eag-related quality (Erg) potassium channels. Moreover, Eag1 is thought to be an imperative marker for a few distinct tumors. Astemizole hinders Eag1 and Erg channel action, and in cells communicating the Eag1 channel it diminishes tumor cell expansion in vitro and in vivo. It ought to be noticed that some cardiovascular reactions have been reported for astemizole in a couple of uncommon cases. Nevertheless, astemizole remains as an extremely encouraging hostile to malignancy apparatus on the grounds that it shows anti-proliferative mechanisms, may serve as the basis to synthesize new anti-cancer agents, and has been previously administered clinically. [1]
Reference:
1. Astemizole: an old anti-histamine as a new promising anti-cancer drug. Anticancer Agents Med Chem. 2011 Mar;11(3):307-14.
| Cas No. | 68844-77-9 | SDF | |
| 别名 | 阿司咪唑; R 43512 | ||
| 化学名 | 1-(4-fluorobenzyl)-N-(1-(4-methoxyphenethyl)piperidin-4-yl)-1H-benzo[d]imidazol-2-amine | ||
| Canonical SMILES | FC1=CC=C(C=C1)CN2C(NC3CCN(CCC(C=C4)=CC=C4OC)CC3)=NC5=CC=CC=C25 | ||
| 分子式 | C28H31FN4O | 分子量 | 458.57 |
| 溶解度 | ≥ 11.5mg/mL in DMSO with gentle warming | 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 | 2.1807 mL | 10.9035 mL | 21.8069 mL |
| 5 mM | 0.4361 mL | 2.1807 mL | 4.3614 mL |
| 10 mM | 0.2181 mL | 1.0903 mL | 2.1807 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。