| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Vernakalant targets sodium (Na+) and potassium (K+) channels. It is a mixed voltage- and frequency-dependent blocker of these channels. By blocking atrial potassium channels, it prolongs repolarization and terminates atrial fibrillation. Its atrial selectivity may reduce the risk of ventricular proarrhythmia.
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| ln Vitro |
Since vernakalant starts to block channel current very quickly following depolarization, blockade of Kv1.5 by vernakalant hydrochloride is mediated after channel activation; nonetheless, there is minimal evidence of channel stasis. obstruction caused by breathing or "tonic" After channel opening in the presence of 10 μM Vernakalant, there was an obvious and quick blocking, and steady-state current levels were quickly achieved. The most significant result was a 25-fold reduction in the effectiveness of vernakalant, which was centered on I502A and had an IC50 of 329±19 μM (n=4–10) compared to 13.4±0.9 μM (n=5-23) for the control group. Smaller potency reductions, ranging from three to four times, were seen at Kv1.5 in V505A, I508A, T480A, and C500A. In our research, I508Y raised Vernakalant's IC50 at Kv1.5 to 24.7 μM, which is once more in line with the hERG value that has been published [1].
In vitro, vernakalant blocks sodium and potassium channels in a voltage- and frequency-dependent manner. It prolongs the atrial effective refractory period and terminates re-entrant arrhythmias. Its atrial selectivity has been demonstrated in electrophysiological studies. |
| ln Vivo |
Vernakalant is used in vivo for the acute conversion of atrial fibrillation. It is administered intravenously at doses of 2 to 5 mg/kg. It has been shown to be effective in terminating acute atrial fibrillation in humans. Its atrial selectivity may reduce the risk of ventricular proarrhythmia.
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| Enzyme Assay |
Vernakalant is an ion channel blocker, and its in vitro activity is assessed in electrophysiological assays. In a typical assay, the compound is applied to cells expressing sodium or potassium channels, and the effect on ion currents is measured using patch-clamp techniques. The voltage- and frequency-dependence of block is assessed.
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| Cell Assay |
Vernakalant is dissolved in DMSO and applied to cultured cells at concentrations ranging from 1 nM to 10 µM. The effect on ion currents is measured using patch-clamp techniques.
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| ADME/Pharmacokinetics |
Vernakalant HCl has a molecular weight of 385.93 g/mol and a molecular formula of C20H32ClNO4. It is an investigational antiarrhythmic agent. The compound is typically stored as a powder at -20°C for long-term stability. Vernakalant HCl is also known as RSD1235.
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| Toxicity/Toxicokinetics |
Vernakalant HCl has a manageable toxicity profile. Common side effects include dysgeusia (taste disturbance), sneezing, and paresthesia. Hypotension and bradycardia can occur. No significant hepatotoxicity or nephrotoxicity has been reported.
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| References |
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| Additional Infomation |
Drug Indication
For the rapid conversion of recently diagnosed adult atrial fibrillation to sinus rhythm: Suitable for non-surgical patients: atrial fibrillation. Vernakalant HCl is an investigational drug for the acute conversion of atrial fibrillation. It is a mixed voltage- and frequency-dependent blocker of sodium (Na+) and potassium (K+) channels. Like other class III antiarrhythmics, vernakalant blocks atrial potassium channels, thereby prolonging repolarization. Vernakalant HCl is a mixed ion channel blocker that can terminate acute atrial fibrillation (AF) in humans at 2 to 5 mg/kg. |
| Molecular Formula |
C20H32CLNO4
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|---|---|
| Molecular Weight |
385.9254
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| Exact Mass |
385.202
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| CAS # |
748810-28-8
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| Related CAS # |
Vernakalant;794466-70-9
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| PubChem CID |
9930048
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| Appearance |
White to light yellow solid powder
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| LogP |
3.38
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
26
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| Complexity |
394
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| Defined Atom Stereocenter Count |
3
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| SMILES |
COC1=C(C=C(C=C1)CCO[C@@H]2CCCC[C@H]2N3CC[C@H](C3)O)OC.Cl
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| InChi Key |
JMHYCBFEEFHTMK-IIUXMCBISA-N
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| InChi Code |
InChI=1S/C20H31NO4.ClH/c1-23-19-8-7-15(13-20(19)24-2)10-12-25-18-6-4-3-5-17(18)21-11-9-16(22)14-21;/h7-8,13,16-18,22H,3-6,9-12,14H2,1-2H3;1H/t16-,17-,18-;/m1./s1
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| Chemical Name |
(3R)-1-[(1R,2R)-2-[2-(3,4-dimethoxyphenyl)ethoxy]cyclohexyl]pyrrolidin-3-ol;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~129.56 mM)
H2O : ~50 mg/mL (~129.56 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.48 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.48 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (129.56 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5911 mL | 12.9557 mL | 25.9114 mL | |
| 5 mM | 0.5182 mL | 2.5911 mL | 5.1823 mL | |
| 10 mM | 0.2591 mL | 1.2956 mL | 2.5911 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
A Pilot Phase II, Randomised, Double-blind, Placebo-controlled, Multi-centred Safety, Tolerability and Preliminary Efficacy
CTID: null
Phase: Phase 2 Status: Completed
Date: 2006-02-02
Products are for research use only; We do not sell to patients
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