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Merck
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文件

M5060

Sigma-Aldrich

E-4031

≥98% (HPLC), lyophilized powder

别名:

N-[4-[[1-[2-(6-甲基-2-吡啶基)乙基]-4-哌啶基]羰基]苯基]甲磺酰胺 二盐酸盐

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About This Item

经验公式（希尔记法）:
C21H27N3O3S · 2HCl
CAS号:
113559-13-0
分子量:
474.44
MDL號碼:
MFCD01754739
分類程式碼代碼:
12352207
PubChem物質ID:
329818000
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

lyophilized powder

儲存條件

desiccated

技術

cell culture | embryo: suitable

顏色

white

溶解度

H2O: soluble

儲存溫度

−20°C

SMILES 字串

Cl.Cl.Cc1cccc(CCN2CCC(CC2)C(=O)c3ccc(NS(C)(=O)=O)cc3)n1

InChI

1S/C21H27N3O3S.2ClH/c1-16-4-3-5-19(22-16)12-15-24-13-10-18(11-14-24)21(25)17-6-8-20(9-7-17)23-28(2,26)27;;/h3-9,18,23H,10-15H2,1-2H3;2*1H

InChI 密鑰

ZQBNWMFBOSOOLX-UHFFFAOYSA-N

相关类别

應用

E-4031 已用作：
  • 人类诱导多能干细胞衍生的心肌细胞（hiPSC-CMs）中的人类ether-a-go-go基因（hERG）阻断剂
  • 长QT综合征（LQTS）诱导的多能干细胞（iPSC）胚状体的IKr阻滞剂
  • 大鼠心室肌细胞中的IKr阻滞剂

生化／生理作用

E-4031是一种抗心律不齐药物，属于III类。它是一种甲磺酰苯胺化合物，可有效治疗心律不齐并调节心室纤颤。E-4031介导转基因长QT 1型（LQT1）兔的动作电位持续时间（action potential duration ，APD）延长。人类 ether-a-go-go相关基因（hERG）中的异亮氨酸突变消除了其与E-4031的相互作用。
E-4031可选择性封闭hERG K+通道。

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。

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

個人防護裝備

Eyeshields, Gloves, type N95 (US)

分析证书(COA)

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Impaired inactivation of L-Type Ca2+ current as a potential mechanism for variable arrhythmogenic liability of HERG K+ channel blocking drugs
Kim JG, et al.
PLoS ONE, 11(3), e0149198-e0149198 (2016)
Susann Björk et al.
Frontiers in physiology, 8, 884-884 (2017-11-23)
Current cardiac drug safety assessments focus on hERG channel block and QT prolongation for evaluating arrhythmic risks, whereas the optogenetic approach focuses on the action potential (AP) waveform generated by a monolayer of human cardiomyocytes beating synchronously, thus assessing the
Dissociation of E-4031 from the HERG channel caused by mutations of an amino acid results in greater block at high stimulation frequency
Ishii K, et al.
Cardiovascular Research, 57(3), 651-659 (2003)
Masataka Fujiwara et al.
PloS one, 6(2), e16734-e16734 (2011-03-03)
Induced pluripotent stem cells (iPSCs) are novel stem cells derived from adult mouse and human tissues by reprogramming. Elucidation of mechanisms and exploration of efficient methods for their differentiation to functional cardiomyocytes are essential for developing cardiac cell models and
Anna L Lahti et al.
Disease models & mechanisms, 5(2), 220-230 (2011-11-05)
Long QT syndrome (LQTS) is caused by functional alterations in cardiac ion channels and is associated with prolonged cardiac repolarization time and increased risk of ventricular arrhythmias. Inherited type 2 LQTS (LQT2) and drug-induced LQTS both result from altered function
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