Nifekalant
Based on 1 Customer Validation
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.
- Purity: 98.22%
- CAS No.: 130636-43-0
- Formula: C19H27N5O5
- Molecular Weight:405.45
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
Cellular Effect
|
Cell Line
|
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
|
[PMID: 23241029] |
| HEK293 | IC50 |
1.1 μM
Compound: nifekalant
|
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
|
[PMID: 23241029] |
| HEK293 | IC50 |
10.3 μM
Compound: nifekalant
|
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
|
[PMID: 23241029] |
| HEK293 | IC50 |
146 μM
Compound: nifekalant
|
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
|
[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
|
[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
|
[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] |
In Vitro
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.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 130636-43-0
-
Appearance Solid
-
Molecular Weight 405.45
-
Formula C19H27N5O5
-
Color White to off-white
-
SMILES
O=C1N(C)C(C=C(NCCN(CCO)CCCC2=CC=C([N+]([O-])=O)C=C2)N1C)=O
-
Synonyms
MS-551 free base
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 62.5 mg/mL (154.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
0.1 M HCl : 12.5 mg/mL (30.83 mM; Need ultrasonic)
H2O : 0.98 mg/mL (2.42 mM; ultrasonic and warming and heat to 60°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (271 KB)
-
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
-
Handling Instructions (2659 KB)
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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / 0.1 M HCl / DMSO | 1 mM | 2.4664 mL | 12.3320 mL | 24.6640 mL | 61.6599 mL |
| 0.1 M HCl / DMSO | 5 mM | 0.4933 mL | 2.4664 mL | 4.9328 mL | 12.3320 mL |
| 10 mM | 0.2466 mL | 1.2332 mL | 2.4664 mL | 6.1660 mL | |
| 15 mM | 0.1644 mL | 0.8221 mL | 1.6443 mL | 4.1107 mL | |
| 20 mM | 0.1233 mL | 0.6166 mL | 1.2332 mL | 3.0830 mL | |
| 25 mM | 0.0987 mL | 0.4933 mL | 0.9866 mL | 2.4664 mL | |
| 30 mM | 0.0822 mL | 0.4111 mL | 0.8221 mL | 2.0553 mL | |
| DMSO | 40 mM | 0.0617 mL | 0.3083 mL | 0.6166 mL | 1.5415 mL |
| 50 mM | 0.0493 mL | 0.2466 mL | 0.4933 mL | 1.2332 mL | |
| 60 mM | 0.0411 mL | 0.2055 mL | 0.4111 mL | 1.0277 mL | |
| 80 mM | 0.0308 mL | 0.1541 mL | 0.3083 mL | 0.7707 mL | |
| 100 mM | 0.0247 mL | 0.1233 mL | 0.2466 mL | 0.6166 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Nifekalant Related Classifications
HY-B0772 Related Classifications
Powered by Bioz