E-4031 (hydrochloride)

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Cat No: 15203

Biochemicals - Ion Channel Modulation

Voltage-gated potassium ERG channels (Kv11.1), encoded by the ether-a-go-go related gene, mediate the inwardly rectifying potassium (K+) current that repolarizes myocardial cells, gut smooth muscle cells, and interstitial cells of Cajal.{24506} E-4031 ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

N-[4-[[1-[2-(6-methyl-2-pyridinyl)ethyl]-4-piperidinyl]carbonyl]phenyl]-methanesulfonamide, dihydrochloride

Correlated keywords:

113558-89-7 voltage-gated voltage gated potassiums ERGs channels Kv11.1 Kvs Kv-11.1 11.1 ether-a-go-go ether a go related genes hERG IKr K+ methanesulfonanilide class III antiarrhythmic anti-arrhythmic anti arrhythmic agents cardiac actions potential duration ADP channel blockers blocks blocking 1 2 3 one two three ERG-1 ERG-2 ERG-3 ERG1 ERG2 ERG3 torsade de long QT sydromes types 2 LQT2 cardiac diseases intervals E4031 E 4031 HCl ions pumps inhibitors inhibits inhibitions cardiology cardio

Product Overview:
Voltage-gated potassium ERG channels (Kv11.1), encoded by the ether-a-go-go related gene, mediate the inwardly rectifying potassium (K+) current that repolarizes myocardial cells, gut smooth muscle cells, and interstitial cells of Cajal.{24506} E-4031 is a methanesulfonanilide class III antiarrhythmic agent that prolongs cardiac action potential duration by blocking ERG K+ channels (IC50 = 29 nM).{24130,24505} E-4031 inhibits the ERG1, ERG2, and ERG3 isoforms with KD values of 99, 116, and 193 nM, respectively.{24503} However, at higher μM concentrations E-4031 can demonstrate pro-arrhythmic activity, inducing early after depolarizations (prolonged repolarization) in cell models and torsade de pointes in animal models.{24131} E-4031 has been used to pharmacologically rescue misprocessed ERG in long QT syndrome type 2, an autosomal dominant cardiac disease associated with prolongation of the QT interval and torsade de pointes.{24504}

Size	5 mg
Shipping	dry ice
CAS Number	113559-13-0
Molecular Formula	C₂₁H₂₇N₃O₃S • 2HCl
SMILES	O=C(C1CCN(CCC2=CC=CC(C)=N2)CC1)C3=CC=C(NS(C)(=O)=O)C=C3.Cl.Cl
Molecular Weight	474,4
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.39
UNSPSC code	12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

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ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.