M5060
E-4031
≥98% (HPLC), lyophilized powder
동의어(들):
N-[4-[[1-[2-(6-Methyl-2-pyridinyl)ethyl]-4-piperidinyl]carbonyl]phenyl]methanesulfonamide dihydrochloride
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모든 사진(1)
About This Item
실험식(Hill 표기법):
C21H27N3O3S · 2HCl
CAS Number:
Molecular Weight:
474.44
MDL number:
UNSPSC 코드:
12352207
PubChem Substance ID:
NACRES:
NA.77
추천 제품
Quality Level
분석
≥98% (HPLC)
양식
lyophilized powder
저장 조건
desiccated
기술
cell culture | embryo: suitable
색상
white
solubility
H2O: soluble
저장 온도
−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
애플리케이션
E-4031 has been used as:
- human ether-a-go-go-related gene (hERG) blocker in human-induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs)
- IKr blocker in long QT syndrome (LQTS) induced pluripotent stem (iPSCs) embryoid bodies
- IKr blocker in rat ventricular myocytes
생화학적/생리학적 작용
E-4031 is a antiarrhythmic drug and belongs to the class III type. It is a methanesulfonanilide compound and is effective in treating arrhythmia and modulates ventricular fibrillation. E-4031 mediates the prolongation of action potential duration (APD) in transgenic long-QT type 1 (LQT1) rabbits. An isoleucine mutation in human ether-a-go-go-related gene (hERG) abolishes its interaction with E-4031.
E-4031 selectively blocks hERG K+ channels.
특징 및 장점
This compound is featured on the Potassium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
개인 보호 장비
Eyeshields, Gloves, type N95 (US)
가장 최신 버전 중 하나를 선택하세요:
이미 열람한 고객
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)
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
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)
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
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)
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