产品说明
包装
5, 25 mg in glass bottle
生化/生理作用
LUF7346 has the ability to enhance the potassium current (IKr) in a heterologous system. It is found to be highly effective than other human ether-a-go-go-related gene (hERG) activators, such as Rottlerin and NS1643.
LUF7346 is a Kv11.1 (hERG) allosteric modulator that prevents proarrhythmic effects caused by hERG blockers in rat ventricular myocyte cultures. LUF7346 reduces Kv11.1 (ERG) affinity toward known Kv11.1 channel blockers dofetilide (Ki for hERG = 4.8 nM without and 12 nM with 10 μM LUF7346) and astemizole (Ki for for hERG = 1.3 nM without and 5.3 nM with 10 μM LUF7346) and effectively suppresses astemizole-induced arrhythmogenic events in a dose-dependent manner among Long-QT syndrome/LQTS (LQT1, JLNS, LQT2) and control isogenic human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs). LUF7346 is shown to slow IKr deactivation and positively shifts IKr inactivation among LQTS and control isogenic hiPSC-CMs without affecting KCNQ1/KCNE1-dependent IKs or L-type calcium current ICaL.
基本信息
经验(实验)分子式 | C20H15BrN2O3 |
分子量 | 411.25 |
NACRES | NA.77 |
产品性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
形式 | powder |
颜色 | white to beige |
溶解性 | DMSO: 10 mg/mL, clear |
储存温度 | 2-8℃ |
SMILES string | O=C(NC1=CC=CN=C1)COC2=CC=C(C(C3=C(Br)C=CC=C3)=O)C=C2 |
安全信息
储存分类代码 | 13 - Non Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |