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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 107707-38-0
- 分子式: C18H20Cl2N4O2
- 分子量:395.28
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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.
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.
化学情報
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CAS 番号 107707-38-0
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分子量 395.28
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
RS-87337 関連分類
HY-113841 関連分類
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- 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