1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Calcium Channel Potassium Channel
  3. CPU-228

CPU-228 是一种复合 III 类抗心律失常剂。CPU-228 可浓度依赖性地阻滞延迟整流钾通道的快速组分 50 (IKr) 和 L 型钙通道 (ICa,L) 的活性,其中对 I(Ca,L) 电流的 IC50 为 0.909 μM。CPU-228 可产生负性肌力作用,在离体左心房中诱导轻度、非频率依赖性的有效不应期 (ERP) 延长。CPU-228 可降低麻醉兔的尖端扭转型室性心动过速 (TDP) 发生率,抑制大鼠中缺血/再灌注诱导的心律失常。CPU-228 可用于尖端扭转型室性心动过速的相关研究。

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CPU-228

CPU-228 Chemical Structure

CAS No. : 446877-42-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CPU-228 is a complex class III antiarrhythmic agent. CPU-228 concentration-dependently blocks the activities of the rapid component 50 of the delayed rectifier potassium channel (IKr) and the L-type calcium channel (ICa,L), with an IC50 value of 0.909 μM for ICa,L current. CPU-228 produces negative inotropic effects and induces mild, non-frequency-dependent prolongation of the effective refractory period (ERP) in isolated left atria. CPU-228 reduces the incidence of torsades de pointes (TDP) in anesthetized rabbits and inhibits ischemia/reperfusion-induced arrhythmias in rats. CPU-228 can be used in studies related to torsades de pointes[1].

IC50 & Target[1]

L-type calcium channel

 

IKr

 

体外研究
(In Vitro)

CPU-228 (0.01-1 μM) 可浓度依赖性地阻断豚鼠离体心室肌细胞中的 IKr,且不改变 IKs 或 IK1 的活性[1]
CPU-228 (0.33-10 μM) 可浓度依赖性地阻断豚鼠离体心室肌细胞中的 ICa,L,其 IC50 为 0.909 μM;还可通过将稳态失活曲线移向更负电位来改变 ICa,L 的动力学特征,且不影响其激活特性[1]
CPU-228 (3.3 μM; 5 min) 可显著抑制大鼠离体心室肌细胞的收缩期胞质钙瞬变,且不改变舒张期钙水平或钙瞬变衰减动力学[1]
CPU-228 (10 nM-100 μM; 15 min) 可浓度依赖性地延长豚鼠离体左心房的 ERP,且无逆向频率依赖性;在 0.5-2.0 Hz 的起搏频率范围内,100 μM 浓度下可产生 23%-24%的延长作用[1]
CPU-228 (10 nM-100 μM) 对豚鼠离体左心房具有浓度依赖性负性肌力作用,其 IC50 为 69.2 μM,且在 100 μM 时可显著降低收缩力[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

426.53

Formula

C23H26N2O4S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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