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Merck
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A2861

Sigma-Aldrich

阿司咪唑

≥98% (HPLC)

别名:

1-（4-氟苄基）-2-（1-[4-甲氧基苯乙基] 哌啶-4-基）氨基苯并咪唑

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About This Item

经验公式（希尔记法）:
C28H31FN4O
CAS号:
68844-77-9
分子量:
458.57
EC 号:
272-441-9
MDL编号:
MFCD00153919
UNSPSC代码:
41121800
PubChem化学物质编号:
329770802
NACRES:
NA.77

方案

≥98% (HPLC)

表单

powder

储存条件

desiccated
protect from light

溶解性

DMSO: >20 mg/mL

创始人

Johnson & Johnson

储存温度

2-8°C

SMILES字符串

COc1ccc(CCN2CCC(CC2)Nc3nc4ccccc4n3Cc5ccc(F)cc5)cc1

InChI

1S/C28H31FN4O/c1-34-25-12-8-21(9-13-25)14-17-32-18-15-24(16-19-32)30-28-31-26-4-2-3-5-27(26)33(28)20-22-6-10-23(29)11-7-22/h2-13,24H,14-20H2,1H3,(H,30,31)

InChI key

GXDALQBWZGODGZ-UHFFFAOYSA-N

基因信息

human ... HRH1(3269)

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生化/生理作用

阿司咪唑是一种强效 hERG 钾通道阻断剂（IC 50 为 0.9 nM），可用作药理学分子伴侣，以纠正折叠缺陷并恢复一些 hERG 通道突变形式的蛋白功能。它还被研究用于治疗疟疾、癌症中的 hERG 和 hEAG 通道功能以及作为第二代抗组胺药 H-1 拮抗剂。
阿司咪唑是一种强效 hERG 钾通道阻滞剂（IC 50 为 0.9 nM）。

特点和优势

该化合物在受体分类和信号转导手册的钾通道页面上有重点介绍。想要浏览手册的其他页面， 请单击此处。
该化合物由 Johnson & Johnson 开发。如需浏览其他制药公司开发的化合物和批准的药物/候选药物列表，请点击此处。

象形图

Exclamation mark
GHS07

警示用语：

Warning

危险声明

H315,H319,H335

危险分类

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

靶器官

Respiratory system

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000404998
0000404998
0000353187
0000353187
0000336603

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Tjøstil Vlaar et al.
Angewandte Chemie (International ed. in English), 51(52), 13058-13061 (2012-11-20)
O(2) in, H(2)O out: Various diamines and related bisnucleophiles readily undergo oxidative isocyanide insertion with Pd(OAc)(2) (1 mol %) as the catalyst and O(2) as the terminal oxidant to give a diverse array of medicinally relevant N heterocycles. The utility
Chitalu C Musonda et al.
Bioorganic & medicinal chemistry letters, 19(2), 481-484 (2008-12-05)
A dual activity, conjugated approach has been taken to form hybrid molecules of two known antimalarial drugs, chloroquine (CQ) and the non-sedating H1 antagonist astemizole. A variety of linkers were investigated to conjugate the two agents into one molecule. Compounds
M F Nilsson et al.
Reproductive toxicology (Elmsford, N.Y.), 29(2), 156-163 (2010-02-11)
Drugs blocking the potassium current IKr of the heart (via hERG channel-inhibition) have the potential to cause hypoxia-related teratogenic effects. However, this activity may be missed in conventional teratology studies because repeat dosing may cause resorptions. The aim of the
Fumimasa Nomura et al.
Journal of nanobiotechnology, 9, 39-39 (2011-09-21)
Conventional in vitro approach using human ether-a-go-go related gene (hERG) assay has been considered worldwide as the first screening assay for cardiac repolarization safety. However, it does not always oredict the potential QT prolongation risk or pro-arrhythmic risk correctly. For
K A Rao et al.
Mayo Clinic proceedings, 69(6), 589-593 (1994-06-01)
An overdose of astemizole predisposes the myocardium to ventricular dysrhythmias, including torsades de pointes. Herein we describe a case of astemizole-induced torsades de pointes ventricular tachycardia and also review previous case reports in the literature. All the patients were young
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