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Merck
CN

A2861

阿司咪唑

≥98% (HPLC), hERG potassium channel blocker, powder

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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关于此项目

经验公式(希尔记法):
C28H31FN4O
化学文摘社编号:
分子量:
458.57
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
41121800
EC Number:
272-441-9
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Storage condition:
desiccated
protect from light
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产品名称

阿司咪唑, ≥98% (HPLC)

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

SMILES string

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

assay

≥98% (HPLC)

form

powder

storage condition

desiccated
protect from light

solubility

DMSO: >20 mg/mL

originator

Johnson & Johnson

storage temp.

2-8°C

Quality Level

Gene Information

human ... HRH1(3269)

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Biochem/physiol Actions

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)。

Features and Benefits

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

pictograms

Exclamation mark

signalword

Warning

Hazard Classifications

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

target_organs

Respiratory system

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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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
Kiem Vu et al.
Medical mycology, 48(2), 255-262 (2009-07-03)
Cryptococcus neoformans is the leading cause of fungal meningitis, a life-threatening infection that occurs predominately in immuocompromised patients. Current drug therapies are limited to amphotericin B, flucytosine and the azoles since the echinocandins have no demonstrated activity against yeast like
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

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