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
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352207
MDL number:
Assay:
≥98% (HPLC)
Form:
lyophilized powder
Quality Level
assay
≥98% (HPLC)
form
lyophilized powder
storage condition
desiccated
technique(s)
cell culture | embryo: suitable
color
white
solubility
H2O: soluble
storage temp.
−20°C
SMILES string
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
Application
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
Biochem/physiol Actions
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。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
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)
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)
Identification of small-molecule ion channel modulators in C. elegans channelopathy models
Jiang Q, et al.
Nature Communications, 9(1), 3941-3941 (2018)
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| M5060-.1MG | 04061834059493 |
| M5060-.5MG | 04061834059509 |
| M5060-1MG | 04061834059516 |