Nifekalant
Nifekalant (MS-551), a class III antiarrhythmic agent, is a IKr potassium channel blocker with an IC50 of 10 μM. Nifekalant can be used for refractory ventricular tachyarrhythmias research.
For research use only. We do not sell to patients.
- CAS No.: 130636-43-0
- Formula: C19H27N5O5
- Molecular Weight:405.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>300 μM
Compound: nifekalant
|
Inhibition of human OCT1-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Inhibition of human OCT1-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
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[PMID: 23241029] |
| HEK293 | IC50 |
1.1 μM
Compound: nifekalant
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Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis
Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis
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[PMID: 23241029] |
| HEK293 | IC50 |
10.3 μM
Compound: nifekalant
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Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
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[PMID: 23241029] |
| HEK293 | IC50 |
146 μM
Compound: nifekalant
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Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
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[PMID: 23241029] |
| HEK293 | IC50 |
2.7 μM
Compound: nifekalant
|
Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
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[PMID: 23241029] |
| HEK293 | IC50 |
6.5 μM
Compound: nifekalant
|
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
|
[PMID: 23241029] |
| HEK293 | IC50 |
6.5 μM
Compound: nifekalant
|
Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay
Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay
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[PMID: 23241029] |
| MDCK-II | IC50 |
0.65 μM
Compound: nifekalant
|
Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis
Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis
|
[PMID: 23241029] |
Nifekalant interacts with the cardiac M2 and the peripheral M3 receptors with a Ki value of 27 and 74 mM, respectively. Nifekalant dose dependently blocks HERG channels with an IC50 value of 7.9 mM, but Nifekalant does not block minK currents in the Xenopus oocyte expression system. Nifekalant blocks HERG channels mainly in their open state in a frequency dependent manner. As a pure K+ channel blocker, Nifekalant does not have negative inotropic effects which amiodarone has via a β-blocking action and does not affect cardiac conduction[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 130636-43-0
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Molecular Weight 405.45
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Formula C19H27N5O5
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SMILES
O=C1N(C)C(C=C(NCCN(CCO)CCCC2=CC=C([N+]([O-])=O)C=C2)N1C)=O
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Synonyms
MS-551 free base
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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.
Purity & Documentation
References
[1]. Lü-Pei Du, et al. The pharmacophore hypotheses of I(Kr) potassium channel blockers: novel class III antiarrhythmic agents. Bioorg Med Chem Lett. 2004 Sep 20;14(18):4771-7. [Content Brief]
[2]. Ioannis N Pantazopoulos, et al. Nifekalant in the treatment of life-threatening ventricular tachyarrhythmias. World J Cardiol. 2011 Jun 26;3(6):169-76. [Content Brief]
[3]. J Chen, et al. IK independent class III actions of MS-551 compared with sematilide and dofetilide during reperfusion in anaesthetized rats. Br J Pharmacol. 1996 Nov;119(5):937-42. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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