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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
Sematilide (formerly known as CK-1752) is a novel class III antiarrhythmic agent. It acts as a selective delayed rectifier K+ current (IKr) channel blocker. I The sematilide-sensitive current, which was recorded by means of a triangular voltage command, showed a strong inward rectification and had a peak at about -40 mV, suggesting that sematilide inhibits the rapidly activating delayed rectifier K+ current. The Ca2+-independent transient K+ and the inward rectifier K+ currents were not affected significantly by application of 100 microM sematilide. Moreover, voltage-dependent Na+ and Ca2+ currents were not affected significantly by 100 microM sematilide. These findings indicate that sematilide selectively blocks the rapidly activating delayed rectifier K+ current in atrial myocytes and provide evidence supporting the usefulness of the drug as a class III antiarrhythmic agent.
ln Vitro |
Applying 10, 30, 100, and 300 μM of sematilide inhibits delayed rectifier K+ current (IC50=25 μM) in a concentration-dependent manner [1].
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ln Vivo |
In dogs with arrhythmia models, simalide (0.3–1.0 mg/kg, intravenous injection) works well [2].
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Animal Protocol |
Animal/Disease Models: Mongrel dogs of either sex (body weight 10-18 kg) [2]
Doses: 0.3, 1, 3 and 10 mg/kg Route of Administration: intravenous (iv) (iv)infusion Experimental Results: 0.3 and 3.0 mg/kg demonstrated antirhythmic effects Abnormal effects. |
References |
[1]. Ishii Y, et al. Effects of Sematilide, a novel class III antiarrhythmic agent, on membrane currents in rabbit atrial myocytes. Eur J Pharmacol. 1997 Jul 23;331(2-3):295-302.
[2]. Stanley S. Greenberg, et al. Pharmacology of Sematilide, a non-quaternary class III antiarrhythmic agent. |
Molecular Formula |
C14H24CLN3O3S
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Molecular Weight |
349.87
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Elemental Analysis |
C, 48.06; H, 6.91; Cl, 10.13; N, 12.01; O, 13.72; S, 9.16
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CAS # |
101526-62-9
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Related CAS # |
Sematilide;101526-83-4
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Appearance |
Solid powder
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SMILES |
O=C(NCCN(CC)CC)C1=CC=C(NS(=O)(C)=O)C=C1.[H]Cl
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Chemical Name |
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Synonyms |
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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. |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: 0.5 mg/mL (1.43 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 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: 0.5 mg/mL (1.43 mM) 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; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 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: 0.5 mg/mL (1.43 mM) in 10% DMSO + 90% Corn Oil (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 | 2.8582 mL | 14.2910 mL | 28.5820 mL | |
5 mM | 0.5716 mL | 2.8582 mL | 5.7164 mL | |
10 mM | 0.2858 mL | 1.4291 mL | 2.8582 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.