PD-118057
规格
| Cas Number | 313674-97-4 |
| 规格或纯度 | Moligand™, ≥97% |
| 级别 | Moligand™ |
| 纯度 | ≥97% |
| 包装 | 100mg 或 50mg 或 10mg 或 1mg 或 5mg 或 25mg |
产品信息
| 别名 | 2-[[4-[2-(3,4-二氯苯基)乙基]苯基]氨基]苯甲酸 |
| 品牌 | 阿拉丁 |
| Action Type | 激活剂 |
| Mechanism Of Action | K 激活程序 v11.1 |
| 溶解性 | 溶于DMSO, 最高浓度 (mg/mL): 38.63, 最高浓度(mM): 100；溶于ethanol, 最高浓度 (mg/mL): 7.73, 最高浓度(mM): 20 |
| 简短描述 | 选择性KV11.1（hERG）通道激活剂 |
| 英文简短描述 | Selective KV11.1 (hERG) channel activator |
| 过滤标签 | Kv11.1 Activator,Potassium Channel,膜转运器/离子通道,钾离子通道 |
| 储存温度 | 避光,-20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 物理形态 | 固体 |
| 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。 |
| 英文描述 |
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. 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.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. |