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NS3623

Catalog No. T16347   CAS 343630-41-1

NS3623 is an activator of human ether-a-go-go-related gene potassium channels. NS3623 has a dual mode of action, being an inhibitor of hERG1 channels. NS3623 activates the IKr and Ito currents and has an antiarrhythmic effect.

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NS3623 Chemical Structure
NS3623, CAS 343630-41-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
5 mg In stock $ 80.00
10 mg In stock $ 128.00
25 mg In stock $ 263.00
50 mg In stock $ 428.00
100 mg In stock $ 639.00
1 mL * 10 mM (in DMSO) In stock $ 89.00
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Purity: 98.1%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description NS3623 is an activator of human ether-a-go-go-related gene potassium channels. NS3623 has a dual mode of action, being an inhibitor of hERG1 channels. NS3623 activates the IKr and Ito currents and has an antiarrhythmic effect.
In vitro Administering NS3623 (5 μM) significantly enhances the tail current magnitude in isolated canine cardiomyocytes, corroborating earlier evidence that this compound augments IKr. Specifically, NS3623 boosts IKr tail currents by 60% in normal Mid cells and by 68% in cells cultured for 48 hours, at a +50 mV activating pulse. Furthermore, although the baseline IKr in cells cultured for 48 hours markedly declines compared to freshly isolated cells—from 0.47 ± 0.08 pA/pF to 0.28 ± 0.06 pA/pF—NS3623 application elevates IKr in these cultured Mid cells. An analysis of the current-voltage (I-V) relationship for IKr tail current reveals that NS3623 increases current density in Mid cells cultured for both one and two days.
In vivo NS3623 (30 mg/kg; i.v.; lasting for 3 minutes) shortens the corrected QT interval by 25 +/- 4% in anaesthetized guinea pigs.
NS3623 (50 mg/kg) immediately reduces the QTcF interval and remains obviously shortened for approximately 30 minutes. NS3623 (50 mg/kg) shortens the QT interval by 30 +/- 6% in conscious guinea pigs [1].
Molecular Weight 427.18
Formula C15H10BrF3N6O
CAS No. 343630-41-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 9.17 mg/ml (21.46 mM)

TargetMolReferences and Literature

1. Hansen RS, et al. In vivo effects of the IKr agonist NS3623 on cardiac electrophysiology of the guinea pig. J Cardiovasc Pharmacol. 2008 Jul;52(1):35-41. 2. Diness JG, et al. Antiarrhythmic effect of IKr activation in a cellular model of LQT3. Heart Rhythm. 2009 Jan;6(1):100-6. 3. Calloe K, et al. A dual potassium channel activator improves repolarization reserve and normalizes ventricular action potentials. Biochem Pharmacol. 2016 May 15;108:36-46. 4. Hansen RS, et al. Biophysical characterization of the new human ether-a-go-go-related gene channel opener NS3623 [N-(4-bromo-2-(1H-tetrazol-5-yl)-phenyl)-N'-(3'-trifluoromethylphenyl)urea]. Mol Pharmacol. 2006 Oct;70(4):1319-29.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Bioactive Compounds Library Max Potassium Channel Blocker Library Ion Channel Inhibitor Library NO PAINS Compound Library Bioactive Compound Library Covalent Inhibitor Library Anti-Cancer Compound Library

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Keywords

NS3623 343630-41-1 Membrane transporter/Ion channel Potassium Channel channels midmyocardial cardiomyocytes current ion canine Potassium KcsA Inhibitor inhibit NS 3623 cells Antiarrhythmic effect NS-3623 inhibitor

 

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