Vernakalant Hydrochloride
Based on 3 publication(s) in Google Scholar
Vernakalant hydrochloride is a mixed voltage- and frequency-dependent Na+ and atria-preferred K+ channel blocker. IC50 for block by Vernakalant of wild-type and mutant Kv1.5 channels Fractional block is 13.35±0.93 μM, 0.61±0.03 μM, and 1.63±0.09 μM for Kv1.5 channelwt, Kv1.5 channelI508F, Kv1.5 channelT479A, respectively.
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- Pureté: 99.33%
- CAS No.: 748810-28-8
- Formule: C20H32ClNO4
- Masse moléculaire:385.93
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) Vernakalant Hydrochloride
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Activité biologique
IC50: 13.35±0.93 μM (Kv1.5 channelwt), 0.61±0.03 μM (I508F), 1.63±0.09 μM (Kv1.5 channel T479A)[1]
Block of Kv1.5 by Vernakalant Hydrochloride is mediated after channel activation, because Vernakalant causes a relatively rapid onset of block of channel current upon depolarization but little evidence of resting or “tonic” block of the channel. In the presence of 10 μM Vernakalant, rapid block is apparent after channel opening, and a steady-state current level is rapidly reached. The most important effect is the reduction in potency for Vernakalant centered at I502A, which had an IC50 of 329±19 μM (n=4-10), compared with a control IC50 of 13.4±0.9 μM (n=5-23), which is a 25-fold decrease in potency. V505A, I508A, T480A, and C500A showed lesser reductions in potency on Kv1.5, of between 3- and 4-fold. I508Y in our experiments increased the IC50 for Vernakalant on Kv1.5 to 24.7 μM, again similar to the reported value for hERG[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 748810-28-8
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Appearance Solid
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Masse moléculaire 385.93
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Formule C20H32ClNO4
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Color White to light yellow
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SMILES
COC1=C(OC)C=C(CCO[C@H]2[C@H](N3CC[C@@H](O)C3)CCCC2)C=C1.Cl
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Synonyms
RSD1235 hydrochloride
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Stem Cell Res Ther
JAK2 as a surface marker for enrichment of human pluripotent stem cells-derived ventricular cardiomyocytes. [Abstract]2023 Dec 13;14(1):367. PMID: 38093391 -
Clin Pharmacol Ther
Thorough QT/QTc in a Dish: An In Vitro Human Model That Accurately Predicts Clinical Concentration-QTc Relationships. [Abstract]2019 May;105(5):1175-1186. PMID: 30346629 -
J Pharmacol Sci
Influences of rapid pacing-induced electrical remodeling on pharmacological manipulation of the atrial refractoriness in rabbits. [Abstract]2016 Mar;130(3):170-6. PMID: 27032905
Solvant et solubilité
DMSO : 50 mg/mL (129.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (129.56 mM; Need ultrasonic)
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
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 (6.48 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 (6.48 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 50 mg/mL (129.56 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureté et documentation
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Fiche technique (275 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Eldstrom J, et al. The molecular basis of high-affinity binding of the antiarrhythmic compound Vernakalant (RSD1235) to Kv1.5 channels. Mol Pharmacol. 2007 Dec;72(6):1522-34. [Content Brief]
[2]. Chiba T, et al. Influences of rapid pacing-induced electrical remodeling on pharmacological manipulation of the atrial refractoriness in rabbits. J Pharmacol Sci. 2016 Mar;130(3):170-6. [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 (sealed storage, away from moisture). 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 / H2O | 1 mM | 2.5911 mL | 12.9557 mL | 25.9114 mL | 64.7786 mL |
| 5 mM | 0.5182 mL | 2.5911 mL | 5.1823 mL | 12.9557 mL | |
| 10 mM | 0.2591 mL | 1.2956 mL | 2.5911 mL | 6.4779 mL | |
| 15 mM | 0.1727 mL | 0.8637 mL | 1.7274 mL | 4.3186 mL | |
| 20 mM | 0.1296 mL | 0.6478 mL | 1.2956 mL | 3.2389 mL | |
| 25 mM | 0.1036 mL | 0.5182 mL | 1.0365 mL | 2.5911 mL | |
| 30 mM | 0.0864 mL | 0.4319 mL | 0.8637 mL | 2.1593 mL | |
| 40 mM | 0.0648 mL | 0.3239 mL | 0.6478 mL | 1.6195 mL | |
| 50 mM | 0.0518 mL | 0.2591 mL | 0.5182 mL | 1.2956 mL | |
| 60 mM | 0.0432 mL | 0.2159 mL | 0.4319 mL | 1.0796 mL | |
| 80 mM | 0.0324 mL | 0.1619 mL | 0.3239 mL | 0.8097 mL | |
| 100 mM | 0.0259 mL | 0.1296 mL | 0.2591 mL | 0.6478 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.
Vernakalant Hydrochloride Related Classifications
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