| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
Sotalol D6 HCl, as the deuterated form of sotalol, targets β-adrenergic receptors as a non-selective beta-adrenoceptor blocker. Sotalol also blocks potassium KCNH2 channels, which contributes to its Class III antiarrhythmic properties. The deuterated form has the same pharmacological target profile as the non-deuterated compound.
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| ln Vitro |
Sotalol hydrochloride is an orally active, non-selective competitive β-adrenergic receptor blocker and a potent antiarrhythmic agent. It blocks both β1- and β2-adrenergic receptors and potassium KCNH2 channels, resulting in both Class II and Class III antiarrhythmic effects.
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| ln Vivo |
Sotalol hydrochloride is orally bioavailable and has been used for the treatment of cardiac arrhythmias, including in pediatric populations. The compound's antiarrhythmic effects are mediated through β-adrenoreceptor blockade and prolongation of the cardiac action potential duration via KCNH2 channel blockade.
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| Enzyme Assay |
Sotalol's binding to β-adrenergic receptors can be assessed using radioligand binding assays with membrane preparations from cells expressing β1- and β2-adrenergic receptors. Competition binding experiments are performed with increasing concentrations of sotalol against a fixed concentration of a radiolabeled β-adrenergic receptor ligand. KCNH2 channel blockade can be assessed using patch clamp electrophysiology in cells expressing KCNH2 channels.
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| Cell Assay |
The cellular activity of sotalol is evaluated in cardiomyocyte cell lines or primary cardiomyocytes. Cells are treated with increasing concentrations of sotalol, and β-adrenergic receptor-mediated cAMP production is measured. Antagonist activity is assessed by the compound's ability to block isoproterenol-induced cAMP accumulation. KCNH2 channel blockade is assessed by measuring action potential duration or ion currents using patch clamp techniques.
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| Animal Protocol |
Sotalol is administered orally in animal models for pharmacokinetic and pharmacodynamic studies. In rodent or canine models, blood samples are collected at various time points to measure sotalol concentrations. Electrocardiogram (ECG) parameters such as QT interval prolongation are monitored to assess antiarrhythmic effects.
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| ADME/Pharmacokinetics |
Sotalol D6 HCl has a molecular formula of C12H15D6ClN2O3S and a molecular weight of 314.86 g/mol. It is soluble in DMSO, methanol, and water. The compound is used as an internal standard in analytical method development.
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| Toxicity/Toxicokinetics |
The toxicity profile of sotalol is consistent with that of other β-adrenoreceptor blockers and antiarrhythmic agents. Potential adverse effects may include bradycardia, hypotension, prolongation of QT interval, and proarrhythmia. Specific LD50 values are not extensively detailed.
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| References | |
| Additional Infomation |
Sotalol D6 HCl (CAS# 1246820-85-8) is the deuterium-labeled form of sotalol hydrochloride. Sotalol hydrochloride is an orally bioavailable, non-selective beta-adrenoceptor blocker with antiarrhythmic effects that can be used for pediatric arrhythmias. The deuterated form is used as an analytical standard.
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| Molecular Formula |
C12H14D6N2O3S.HCL
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|---|---|
| Molecular Weight |
314.862
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| Exact Mass |
314.133
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| CAS # |
1246820-85-8
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| Related CAS # |
Sotalol-d6;1246912-17-3
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| PubChem CID |
57369408
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
19
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| Complexity |
330
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[2H]C([2H])([2H])C(C([2H])([2H])[2H])NCC(C1=CC=C(C=C1)NS(=O)(=O)C)O.Cl
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| InChi Key |
VIDRYROWYFWGSY-TXHXQZCNSA-N
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| InChi Code |
InChI=1S/C12H20N2O3S.ClH/c1-9(2)13-8-12(15)10-4-6-11(7-5-10)14-18(3,16)17;/h4-7,9,12-15H,8H2,1-3H3;1H/i1D3,2D3;
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| Chemical Name |
N-[4-[2-(1,1,1,3,3,3-hexadeuteriopropan-2-ylamino)-1-hydroxyethyl]phenyl]methanesulfonamide;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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1760 mL | 15.8801 mL | 31.7601 mL | |
| 5 mM | 0.6352 mL | 3.1760 mL | 6.3520 mL | |
| 10 mM | 0.3176 mL | 1.5880 mL | 3.1760 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.
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