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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Potassium Channel-PD-118057
PD-118057

Chemical Structure : PD-118057

CAS No.: 313674-97-4

PD-118057 (PD 118057;PD118057)

货号: PC-60840Not For Human Use, Lab Use Only.

PD-118057 is a potent, selective hERG potassium channel (Kv11.1) activator that increases peak tail hERG current of 111.1% at 10 uM in HEK293 cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PD-118057 is a potent, selective hERG potassium channel (Kv11.1) activator that increases peak tail hERG current of 111.1% at 10 uM in HEK293 cells.
PD-118057 does not ot affect the voltage dependence and kinetics of gating parameters, and open conformation of the channel, also shows no major effect on I(Na), I(Ca,L), I(K1), and I(Ks).
PD-118057 shortens the action potential duration and QT interval in arterially perfused rabbit ventricular wedge preparation, prevents action potential duration and QT prolongation caused by dofetilide at 3 uM.

物理化学性质&存储条件

分子量 386.272
分子式 C21H17Cl2NO2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-{4-[2-(3,4-dichloro-phenyl)-ethyl]-phenylamino}-benzoic acid

参考文献

1. Zhou J, et al. Mol Pharmacol. 2005 Sep;68(3):876-84. Epub 2005 Jun 23.

2. Patel C, et al. Heart Rhythm. 2008 Apr;5(4):585-90.

3. Perry M, et al. Proc Natl Acad Sci U S A. 2009 Nov 24;106(47):20075-80.

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