Dofetilide, HERG 阻断剂

Potassium Channel Inhibitors
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Compound libraries (12332)

基本描述

别名 多非利特
英文别名 UK-68798 | N-​[4-​[2-​[methyl[2-​[4-​[(methylsulfonyl)​amino]​phenoxy]​ethyl]​amino]​ethyl]​phenyl]​-methanesulfonamide
规格或纯度 Moligand™, 10mM in DMSO
英文名称 Dofetilide
生化机理 多非利特(UK-68798)是一种选择性钾通道((hERG))阻滞剂,属于 III 类抗心律失常药物。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 封闭剂
作用机制 HERG 阻断剂
产品介绍

A potassium channel blocker.

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%

产品属性

ALogP 1.679
hba_count 5
HBD Count 2
Rotatable Bond 11

关联靶点(人)

KCNH1 Tclin 钾电压门控通道亚家族H成员1(Potassium voltage-gated channel subfamily H member 1) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
KCNH2 Tclin 钾电压门控通道亚家族 H 成员 2(Potassium voltage-gated channel subfamily H member 2) (21 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Canonical SMILES CN(CCOC1=CC=C(N[S](C)(=O)=O)C=C1)CCC2=CC=C(N[S](C)(=O)=O)C=C2
分子量 441.56
Reaxy-Rn 3572833
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=3572833&ln=

化学和物理性质

DMSO(mg / mL) Max Solubility 88
DMSO(mM) Max Solubility 199.29
Water(mg / mL) Max Solubility <1

安全和危险性(GHS)

Reaxy-Rn 3572833
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=3572833&ln=

技术规格说明书

Concentration(Compounding value) 9-11(mmol/L)
Record the entire process by video Conform

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
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