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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。
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)
其他客户在看
Impaired inactivation of L-Type Ca2+ current as a potential mechanism for variable arrhythmogenic liability of HERG K+ channel blocking drugs
PLoS ONE, 11(3), e0149198-e0149198 (2016)
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
Dissociation of E-4031 from the HERG channel caused by mutations of an amino acid results in greater block at high stimulation frequency
Cardiovascular Research, 57(3), 651-659 (2003)
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
Pronounced effects of HERG-blockers E-4031 and erythromycin on APD, spatial APD dispersion and triangulation in transgenic long-QT type 1 rabbits
PLoS ONE, 9(9), e107210-e107210 (2014)
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