Dofetilide - Moligand™, 10mM in DMSO , HERG blocker, CAS No.115256-11-6, HERG blocker

CAS: 115256-11-6 Cat. No.: D407756 Molecular Weight: 441.56 EC Number: 638-817-5

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

UK-68798 | N-​[4-​[2-​[methyl[2-​[4-​[(methylsulfonyl)​amino]​phenoxy]​ethyl]​amino]​ethyl]​phenyl]​-methanesulfonamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Dofetilide Dofetilide (UK-68798) is a selective potassium channel ((hERG)) blocker, used as a Class III antiarrhythmic drug.
In vitro

Dofetilide blocks HERG currents in excised macro patches of Xenopus oocytes. Dofetilide (1 μM) reduces the amplitude of IKr to 61% of control currents in guinea pig cardiomyocytes, as measured by 200-ms test pulses and analysis of the deactivating tail currents of IKr. Dofetilide increases apico-basal disparity of repolarization, due to a more marked increase of ERPs in the apex than in the base in the intact canine heart.

In vivo

Dofetilide (100 mg/kg, i.v.) does not suppress automaticity arrhythmias induced by two-stage coronary ligation and epinephrine or the coronary ligation and reperfusion arrhythmias, but suppresses the reentry arrhythmia induced by PES in dogs with old myocardial infarction (MI). Dofetilide also shows antiarrhythmic effect in some dogs with digitalis arrhythmia. Dofetilide increases QT interval and shows negative chronotropic effect like that of other class III drugs, but is different in antiarrhythmic profiles from those of other class III agents such as D-sotalol, E-4031, and MS-551 in that it does not prevent the occurrence of ventricular fibrillation (VF) immediately after coronary reperfusion and has some antiarrhythmic effects on digitalis arrhythmia. Dofetilide causes increased resorptions and the same stage-dependent malformations in Sprague-Dawley rats.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥98%

Specifications

Synonyms

UK-68798 | N-​[4-​[2-​[methyl[2-​[4-​[(methylsulfonyl)​amino]​phenoxy]​ethyl]​amino]​ethyl]​phenyl]​-methanesulfonamide

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Dofetilide (UK-68798) is a selective potassium channel ((hERG)) blocker, used as a Class III antiarrhythmic drug.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

BLOCKER, CHANNEL BLOCKER

Mechanism of action

HERG blocker

Product Properties

• ALogP: 1.8

Names and Identifiers

• Isomeric SMILES: CN(CCC1=CC=C(C=C1)NS(=O)(=O)C)CCOC2=CC=C(C=C2)NS(=O)(=O)C
• WGK Germany: 3
• Molecular Weight: 441.56
• Reaxy-Rn: 3572833
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=3572833&ln=

Associated Targets(Human)

KCNH1 Tclin Potassium voltage-gated channel subfamily H member 1 (1 Activities)

Discover Target: KCNH1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (21 Activities)

Discover Target: KCNH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)