M5060
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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关于此项目
经验公式（希尔记法）:
C21H27N3O3S · 2HCl
化学文摘社编号:
分子量:
474.44
MDL编号:
UNSPSC代码:
12352207
PubChem化学物质编号:
NACRES:
NA.77
质量水平
方案
≥98% (HPLC)
表单
lyophilized powder
储存条件
desiccated
技术
cell culture | embryo: suitable
颜色
white
溶解性
H2O: soluble
储存温度
−20°C
SMILES字符串
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 key
ZQBNWMFBOSOOLX-UHFFFAOYSA-N
应用
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可选择性封闭hERG K+通道。
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。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
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)
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
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
Molecular biology of K+ channels and their role in cardiac arrhythmias
Tristani-Firouzi M, et al.
The American Journal of Medicine, 110(1), 50-59 (2001)
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