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活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
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货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
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D407756-1ml |
1ml |
现货 ![]() |
|
别名 | 多非利特 |
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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. 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 lines: Concentrations: Incubation Time: Powder Purity:≥98% |
ALogP | 1.679 |
---|---|
hba_count | 5 |
HBD Count | 2 |
Rotatable Bond | 11 |
分子类型 | 小分子 |
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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= |
DMSO(mg / mL) Max Solubility | 88 |
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DMSO(mM) Max Solubility | 199.29 |
Water(mg / mL) Max Solubility | <1 |
Reaxy-Rn | 3572833 |
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Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=3572833&ln= |
Concentration(Compounding value) | 9-11(mmol/L) |
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Record the entire process by video | Conform |