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Merck

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:
分子量:
458.57
EC號碼:
MDL號碼:
分類程式碼代碼:
41121800
PubChem物質ID:
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

儲存條件

desiccated
protect from light

溶解度

DMSO: >20 mg/mL

起源

Johnson & Johnson

儲存溫度

2-8°C

SMILES 字串

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 密鑰

GXDALQBWZGODGZ-UHFFFAOYSA-N

基因資訊

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。

特點和優勢

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

象形圖

Exclamation mark

訊號詞

Warning

危險聲明

危險分類

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

標靶器官

Respiratory system

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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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
Andrew M Sawayama et al.
Chemistry (Weinheim an der Bergstrasse, Germany), 15(43), 11723-11729 (2009-09-24)
Herein we demonstrate that a small panel of variants of cytochrome P450 BM3 from Bacillus megaterium covers the breadth of reactivity of human P450s by producing 12 of 13 mammalian metabolites for two marketed drugs, verapamil and astemizole, and one
Astemizole. A nonsedating antihistamine with fast and sustained activity.
M M Janssens
Clinical reviews in allergy, 11(1), 35-63 (1993-01-01)
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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