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PD-118057
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产品介绍
产品介绍
产品信息
抗原名称
0
简单描述
PD-118057 是一种有效的乙醚相关(hERG)钾通道激活剂，对 hERG 不显示活性。PD-118057 通过激活 hERG 通道来抑制膜的兴奋性变化。PD-118057预防和逆转 QT 间期延长，是治疗遗传性或获得性长 QT 综合征和充血性心力衰竭的延迟复极的潜在化合物。
商品描述
PD-118057 is a potent ether associated (hERG) potassium channel activator that shows no activity against hERG. PD-118057 inhibits the excitability of the membrane by activating the hERG channel. PD-118057 is a potential compound for the treatment of delayed repolarization in inherited or acquired long QT syndrome and congestive heart failure.
分子量
386.27
纯度
99.97%
性状
Solid
颜色
Yellow
In vitro(体外研究)
PD-118057 (3 μM and 10 μM) specifically increases hERG current and inhibits action potential duration in guinea pig ventricular muscle in acute isolation of guinea pig cardiomyocytes.[1][2]
PD-118057 (10 μM) counteracts the current inhibition triggered by Dof and Mox while preserving the unaltered 'hump' shape of the IKr current and exhibiting only a marginal increase in the maximum value of the suppressed current.[2]
In vivo(体内研究)
0
背景
别名
0
分子式
C21H17Cl2NO2
CAS号
313674-97-4
密度
1.353 g/cm3 (Predicted)
制备和贮存
溶解方法
DMSO: 90.0 mg/mL (233.0 mM), Sonication is recommended.
存储溶液
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
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