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)
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
Pronounced effects of HERG-blockers E-4031 and erythromycin on APD, spatial APD dispersion and triangulation in transgenic long-QT type 1 rabbits
Ziupa D, et al.
PLoS ONE, 9(9), e107210-e107210 (2014)
Sebastian Schaaf et al.
PloS one, 6(10), e26397-e26397 (2011-10-27)
Human embryonic stem cell (hESC) progenies hold great promise as surrogates for human primary cells, particularly if the latter are not available as in the case of cardiomyocytes. However, high content experimental platforms are lacking that allow the function of
Min Li et al.
Journal of pharmacological sciences, 134(2), 75-85 (2017-06-16)
Human induced pluripotent stem cell (hiPSC)-derived cardiomyocytes hold great potentials to predict pro-arrhythmic risks in preclinical cardiac safety screening, although the hiPSC cardiomyocytes exhibit rather immature functional and structural characteristics, including spontaneous activity. Our physiological characterization and mathematical simulation showed
Daisuke Fukumoto et al.
Journal of cardiology, 71(4), 401-408 (2017-11-18)
Missense mutations in KCNH2, a gene encoding the Kv11.1 channel, cause long QT syndrome (LQTS) type 2 primarily by disrupting the intracellular transport of Kv11.1 to the plasma membrane. The present study aimed to clarify the functional changes by two
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