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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。
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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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 993 | 现货 | |
5 mg | ¥ 2,150 | 现货 | |
10 mg | ¥ 3,290 | 现货 | |
25 mg | ¥ 5,280 | 现货 | |
50 mg | ¥ 7,260 | 现货 | |
100 mg | ¥ 9,790 | 现货 | |
200 mg | ¥ 13,200 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 2,370 | 现货 |
产品描述 | 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. |
体外活性 | 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] |
分子量 | 386.27 |
分子式 | C21H17Cl2NO2 |
CAS No. | 313674-97-4 |
Smiles | OC(=O)c1ccccc1Nc1ccc(CCc2ccc(Cl)c(Cl)c2)cc1 |
密度 | 1.353 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 90.0 mg/mL (233.0 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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