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.
For research use only. We do not sell to patients.
- CAS No.: 446877-42-5
- Formula: C23H26N2O4S
- Molecular Weight:426.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Calcium Channel Isoforms
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Biological Activity
Description
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. Further protocols information, click here.
Chemical Information
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CAS No. 446877-42-5
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Molecular Weight 426.53
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Formula C23H26N2O4S
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SMILES
O=C(N(CCOC1=CC=CC=2C=CC=CC12)CCC3=CC=C(C=C3)NS(=O)(=O)C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- CPU-228
- 446877-42-5
- CPU228
- CPU 228
- Calcium Channel
- Potassium Channel
- rapid component of delayed rectifier potassium channel (I_Kr)
- torsades de pointes
- ventricular myocytes
- inward rectifier potassium channel (I_K1)
- anaesthetized rabbits
- slow component of delayed rectifier potassium channel (I_Ks)
- Na+/Ca2+ exchanger (NCX) currents
- L-type calcium channel (I_Ca,L)
- rats
- sodium currents (I_Na)
- Inhibitor
- inhibitor
- inhibit