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

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.

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CPU-228

CPU-228 Chemical Structure

CAS No. : 446877-42-5

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CPU-228 Related Antibodies

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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Description

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

 

In Vitro

CPU-228 (0.01-1 μM) concentration-dependently blocks IKr in isolated guinea pig ventricular myocytes without altering the activities of IKs or IK1[1].
CPU-228 (0.33-10 μM) concentration-dependently blocks ICa,L in isolated guinea pig ventricular myocytes, with an IC50 of 0.909 μM. It also alters the kinetic properties of ICa,L by shifting the steady-state inactivation curve to more negative potentials, without affecting its activation characteristics[1].
CPU-228 (3.3 μM; 5 min) significantly inhibits systolic cytoplasmic calcium transients in isolated rat ventricular myocytes without altering diastolic calcium levels or the decay kinetics of calcium transients[1].
CPU-228 (10 nM-100 μM; 15 min) concentration-dependently prolongs the ERP of isolated left atria in guinea pigs without reverse frequency dependence; within the pacing frequency range of 0.5-2.0 Hz, it induces a 23%-24% prolongation at the concentration of 100 μM[1].
CPU-228 (10 nM-100 μM) exerts a concentration-dependent negative inotropic effect on isolated left atria of guinea pigs, with an IC50 of 69.2 μM, and significantly reduces contractile force at 100 μM[1].

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

CPU-228 Related Antibodies
Molecular Weight

426.53

Formula

C23H26N2O4S
CAS No.
SMILES

O=C(N(CCOC1=CC=CC=2C=CC=CC12)CCC3=CC=C(C=C3)NS(=O)(=O)C)C
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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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CPU-228 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CPU-228446877-42-5CPU228CPU 228Calcium ChannelPotassium ChannelCa2+ channelsCa channelsKcsArapid component of delayed rectifier potassium channel (I_Kr)torsades de pointesventricular myocytesinward rectifier potassium channel (I_K1)anaesthetized rabbitsslow component of delayed rectifier potassium channel (I_Ks)Na+/Ca2+ exchanger (NCX) currentsL-type calcium channel (I_Ca,L)ratssodium currents (I_Na)Inhibitorinhibitorinhibit

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