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Chemical Structure| 748810-28-8 Chemical Structure| 748810-28-8

Structure of Vernakalant HCl
CAS No.: 748810-28-8

Chemical Structure| 748810-28-8

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Vernakalant HCl prolongs repolarization by blocking atrial potassium channels, it's a class III antiarrhythmics.

Synonyms: RSD1235 hydrochloride; Vernakalant Hydrochloride; RSD1235, RSD-1235, RSD 1235, Vernakalant HCl, Kynapid, Brinavess

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Product Details of Vernakalant HCl

CAS No. :748810-28-8
Formula : C20H32ClNO4
M.W : 385.93
SMILES Code : O[C@H]1CN([C@H]2[C@H](OCCC3=CC=C(OC)C(OC)=C3)CCCC2)CC1.[H]Cl
Synonyms :
RSD1235 hydrochloride; Vernakalant Hydrochloride; RSD1235, RSD-1235, RSD 1235, Vernakalant HCl, Kynapid, Brinavess
MDL No. :MFCD09833303
InChI Key :JMHYCBFEEFHTMK-IIUXMCBISA-N
Pubchem ID :9930048

Safety of Vernakalant HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H312-H315-H319-H332-H335
Precautionary Statements:P261-P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Canine left atrial cells 3, 10, 30 µM 20–30 min To evaluate the effects of Vernakalant on the electrophysiological properties of canine left atria, results showed that Vernakalant significantly prolonged APD50 at 30 µM and exhibited frequency-dependent inhibition of sodium channel-mediated parameters at rapid rates. Circ Arrhythm Electrophysiol. 2012 Apr;5(2):400-8
Canine pulmonary vein sleeve tissue 3, 10, 30 µM 20–30 minutes To evaluate the effects of Vernakalant on electrophysiological parameters in PV sleeves. Results showed Vernakalant at 3-30 μM slightly prolonged APD85 (~10-15 ms), significantly increased ERP, and produced concentration- and rate-dependent depression of sodium channel-mediated parameters (e.g., Vmax). Heart Rhythm. 2012 Mar;9(3):422-9
SIRPA+/CD200+ cardiomyocytes 10 µM 30 minutes To evaluate the effect of vernakalant on ventricular-like cardiomyocytes, results showed that vernakalant had limited to no significant effect on the calcium repolarization duration of SIRPA+/CD200+ population Stem Cell Res Ther. 2023 Dec 13;14(1):367
SIRPA+/JAK2+ cardiomyocytes 10 µM 30 minutes To evaluate the effect of vernakalant on ventricular-like cardiomyocytes, results showed that vernakalant had limited to no significant effect on the calcium repolarization duration of SIRPA+/JAK2+ population Stem Cell Res Ther. 2023 Dec 13;14(1):367

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Human virtual atrial models Virtual atrial models Virtual administration 10 μM and 30 μM Administration started at 2s and continued until 7s Vernakalant was effective in atria presenting long refractoriness (high ICaL density). For short refractoriness, atria with high INa density responded more favourably to amiodarone than flecainide, and the opposite was found in atria with low INa density. J Physiol. 2023 Sep;601(18):4013-4032
Goats Pacing-induced persistent atrial fibrillation model Intravenous infusion 3.7 mg/kg followed by 4.5 mg/kg Cardioversion attempted after 2 weeks of sustained AF To evaluate the cardioversion efficacy of Vernakalant in a goat model of AF, results showed that Vernakalant successfully cardioverted 5 out of 9 goats. Front Pharmacol. 2021 Jan 27;11:608410
Pigs Atrial fibrillation model induced by atrial tachypacing Intravenous infusion 4 mg/kg 10-minute infusion followed by 30-minute monitoring To evaluate the cardioversion effect of vernakalant in a long-term tachypacing-induced AF model Circ Arrhythm Electrophysiol. 2017 Oct;10(10):e005125

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00989001 Atrial Fibrillation Phase 3 Terminated - -
NCT01174160 Atrial Fibrillation Phase 3 Completed - -
NCT01174160 - Completed - -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.59mL

0.52mL

0.26mL

12.96mL

2.59mL

1.30mL

25.91mL

5.18mL

2.59mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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