NS3623
Based on 1 Customer Validation
NS3623 is an activator of human ether-a-go-go-related gene (hERG1/KV11.1) potassium channels. NS3623 activates the IKr and Ito currents and has antiarrhythmic effect. NS3623 has a dual mode of action, being an inhibitor of hERG1 channels.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.0%
- CAS No.: 343630-41-1
- Formule: C15H10BrF3N6O
- Masse moléculaire:427.18
-
Stockage: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]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
-
HY-16916
NS1643hERG Channels Agonist -
HY-15551
E-4031hERG Channels Blocker -
HY-B0232
DofetilideIKr Blocker -
HY-B0112
MinoxidilEndogenous Metabolite -
HY-W020468
LinopirdineM-type K+ current Inhibitor -
HY-108577
XE991 dihydrochlorideKCNQ Channel Blocker -
HY-12496
NS-1619BK Channel Opener -
HY-B0112R
Minoxidil (Standard)Endogenous Metabolite -
HY-B0401
TolbutamideKATP Inhibitor -
HY-B0401R
Tolbutamide (Standard)KATP Inhibitor -
HY-12343
ML277Potassium Channel Activator -
HY-15209
RepaglinideInsulin Secretagogue
Activité biologique
Description
In Vitro
In isolated canine cardiomyocytes, application of NS3623 (5 μM) greatly increases the size of the tail current confirming previous studies demonstrating this drug increased IKr. The effect of NS3623 on IKr recorded from cells kept in culture is evaluated. After 48 h, the magnitude of IKr is greatly reduced compared to freshly isolated cells. Peak IKr tail currents are 0.47 ± 0.08 pA/pF in freshly isolated myocytes and 0.28 ± 0.06 pA/pF in 2 day cultured myocytes. Application of NS3623 increases IKr in cultured Mid cells. Analysis of the current-voltage (I-V) relation of IKr tail current showed that NS3623 increased current density in both 1 day and 2 day cultured Mid cells. On a percentage basis, NS3623 increases IKr tail currents (at +50 mV activating pulse) by 60% in normal Mid cells, and 68% in 48 h cultured cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
NS3623 (50 mg/kg) shortenes the QT interval by 30 +/- 6% in conscious guinea pigs. NS3623 (50 mg/kg) immediately decreases the QTcF interval and remains significantly shortened for approximately 30 minutes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Anesthetized guinea pig[1]
-
Dosage:30 mg/kg
-
Administration:Intravenous injection; lasting for 3 minutes
-
Result:Shortened the corrected QT interval by 25 +/- 4%.
Chemical Information
-
CAS No. 343630-41-1
-
Appearance Solid
-
Masse moléculaire 427.18
-
Formule C15H10BrF3N6O
-
Color White to off-white
-
SMILES
O=C(NC1=CC=CC(C(F)(F)F)=C1)NC2=CC=C(Br)C=C2C3=NNN=N3
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 250 mg/mL (585.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
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: ≥ 2.08 mg/mL (4.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Pureté et documentation
-
Fiche technique (274 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[2]. Diness JG, et al. Antiarrhythmic effect of IKr activation in a cellular model of LQT3. Heart Rhythm. 2009 Jan;6(1):100-6. [Content Brief]
[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. [Content Brief]
[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. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3409 mL | 11.7047 mL | 23.4093 mL | 58.5233 mL |
| 5 mM | 0.4682 mL | 2.3409 mL | 4.6819 mL | 11.7047 mL | |
| 10 mM | 0.2341 mL | 1.1705 mL | 2.3409 mL | 5.8523 mL | |
| 15 mM | 0.1561 mL | 0.7803 mL | 1.5606 mL | 3.9016 mL | |
| 20 mM | 0.1170 mL | 0.5852 mL | 1.1705 mL | 2.9262 mL | |
| 25 mM | 0.0936 mL | 0.4682 mL | 0.9364 mL | 2.3409 mL | |
| 30 mM | 0.0780 mL | 0.3902 mL | 0.7803 mL | 1.9508 mL | |
| 40 mM | 0.0585 mL | 0.2926 mL | 0.5852 mL | 1.4631 mL | |
| 50 mM | 0.0468 mL | 0.2341 mL | 0.4682 mL | 1.1705 mL | |
| 60 mM | 0.0390 mL | 0.1951 mL | 0.3902 mL | 0.9754 mL | |
| 80 mM | 0.0293 mL | 0.1463 mL | 0.2926 mL | 0.7315 mL | |
| 100 mM | 0.0234 mL | 0.1170 mL | 0.2341 mL | 0.5852 mL |
NS3623 Related Classifications
HY-108586 Related Classifications
Powered by Bioz