RS-87337
RS-87337 is an orally active piperazine-amidine hybrid class Ia (inhibiting Vmax, IC50 = 17 μM)/class III (prolonging ADP90, EC15 = 2 μM) antiarrhythmic agent with selectivity for ventricular conduction. RS-87337 inhibits cardiac sodium channel, thereby reducing the maximum depolarization rate of action potential, with moderate onset and recovery kinetics. RS-87337 reduces cardiac outward potassium conductance (I_K), thus prolonging action potential duration. RS-87337 is applicable to research related to arrhythmia, ventricular arrhythmia, ventricular fibrillation, and myocardial ischemia-reperfusion injury.
For research use only. We do not sell to patients.
- CAS No.: 107707-38-0
- Formula: C18H20Cl2N4O2
- Molecular Weight:395.28
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
RS-87337 (0.1-30 μM; 30 min) produces class III (ADP90 prolongation, EC15 = 2 μM) and class Ia (Vmax inhibition, IC50 = 17 μM) antiarrhythmic effects in isolated guinea pig right ventricular papillary muscles, with intermediate sodium channel block kinetics[2].
RS-87337 (10-1000 nM) does not impair baseline function of isolated working rat hearts, and at 1000 nM, it prevents reperfusion-induced ventricular fibrillation and maintains cardiac function following coronary ischemia[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
RS-87337 (1-5 mg/kg; i.v.) significantly reduces the incidence of reperfusion-induced ventricular tachycardia, fibrillation, and mortality in anaesthetized Sprague-Dawley rats[2].
RS-87337 (3-10 mg/kg; i.v.; 15-60 mg/kg; p.o.) reduces ectopic complex incidence in conscious dogs with post-coronary ligation arrhythmia, with rapid activity via i.v. (3, 10 mg/kg) and sustained activity via oral (30, 60 mg/kg) routes[2].
RS-87337 (0.02-5.0 mg/kg; i.v.; cumulative doses) dose-dependently reduces S-T segment elevation during transient myocardial ischemia and speeds reperfusion recovery in anaesthetized beagle dogs without significant cardiodepression[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 107707-38-0
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Molecular Weight 395.28
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Formula C18H20Cl2N4O2
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SMILES
ClC1=CC(NC(N2CCN(CC2)C3=CC=C(C=C3OC)O)=N)=CC(Cl)=C1
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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.
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Cardiac voltage-sensitive optical mapping
Cardiac voltage-sensitive optical mapping records changes in transmembrane potential from cardiac tissue by staining the preparation with a voltage-sensitive dye and imaging fluorescence changes during electrical activation; the resulting optical action potentials can be used to map activation time, action potential duration, conduction velocity, wavefront propagation, and arrhythmia dynamics. The optical signal represents a relative fluorescence change from a tissue volume rather than a single-cell intracellular recording, so spatial resolution, sampling rate, voltage resolution, optical magnification, light penetration, and motion control must be considered together when interpreting optical action potentials.
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Neuronal voltage-sensitive dye imaging
Neuronal voltage-sensitive dye imaging detects membrane-potential-dependent optical changes from dyes associated with neuronal membranes, enabling optical recording of electrical activity from single neurons, dendrites, axons, spines, or neuronal populations in brain slices and cultured neurons. VSD signals are typically reported as fractional fluorescence or absorbance changes over baseline, such as ΔF/F or ΔI/I, and published protocols use high-speed cameras or photodiode arrays because neuronal voltage signals occur on millisecond time scales. Fast VSD imaging can be applied at two common scales: bulk staining of brain slices to measure circuit-level spatiotemporal activity, and single-cell loading or biolistic delivery to record membrane-potential transients from individual neuronal compartments. Optical signals should be interpreted as membrane-potential-related readouts, and validation by simultaneous electrophysiology or pharmacological controls is recommended when the experimen
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Acute brain-slice whole-cell patch-clamp recording
Acute brain-slice whole-cell patch-clamp recording measures membrane voltage or ionic current from visually targeted cells in living brain slices; after giga-seal formation, the membrane under the pipette is ruptured to provide low-resistance electrical access to the cell interior, enabling current-clamp analysis of excitability and voltage-clamp analysis of synaptic or membrane currents. Acute slices preserve local tissue architecture better than dissociated preparations and allow visually guided recording from defined brain regions or fluorescently labeled cells; however, whole-cell access also permits exchange between pipette solution and cytoplasm, so intracellular dialysis must be considered when interpreting signaling-dependent phenomena.
Purity & Documentation
References
[1].
Allely MC, Alps BJ. Effects of the novel class Ia and class III antiarrhythmic agent RS-87337 on myocardial conduction in the anaesthetised dog. Arch Int Pharmacodyn Ther. 1988 Sep-Oct;295:138-46.
[Content Brief]
[2].
Dumez D, et al. Electrophysiologic, antiarrhythmic, and cardioprotective effects of N-[3,5 dichlorophenyl] 4-[4-hydroxy-2-methoxy-phenyl] piperazine carboxamidine dihydrochloride (RS-87337). J Cardiovasc Pharmacol. 1989 Aug;14(2):184-93.
[Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- RS-87337
- 107707-38-0
- RS87337
- RS 87337
- Others
- Sodium Channel
- Potassium Channel
- cardiac potassium conductance
- ventricular conduction
- ventricular fibrillation
- ventricular tachycardia
- beagle dogs
- guinea pig right ventricular papillary muscles
- Sprague-Dawley rats
- cardiac sodium channels
- myocardial ischemia-reperfusion injury
- ectopic complexes
- Inhibitor
- inhibitor
- inhibit