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Submit ReviewDofetilide
Description: KV11.1 (hERG) channel blocker; inhibits rapid delayed rectifier K+ current (IKr)
Alternative Names: Tikosyn,UK 68798
Chemical Name: 1-(4-Methanesulphonamidophenoxy)-2-[N-(4-methanesulphonamidophenethyl)-N-methylamino]ethane
Purity: ≥99% (HPLC)
Biological Activity for Dofetilide
Dofetilide is a selective potassium channel blocker. Blocks KV11.1 (hERG) channels; inhibits the rapid delayed-rectifier K+ current (IKr). Displays class III antiarrhythmic properties.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries for Dofetilide
Dofetilide is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
Technical Data for Dofetilide
| M. Wt | 441.56 |
| Formula | C19H27N3O5S2 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 115256-11-6 |
| PubChem ID | 71329 |
| InChI Key | IXTMWRCNAAVVAI-UHFFFAOYSA-N |
| Smiles | CN(CCC2=CC=C(NS(=O)(C)=O)C=C2)CCOC1=CC=C(NS(=O)(C)=O)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Dofetilide
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 44.16 | 100 |
Preparing Stock Solutions for Dofetilide
The following data is based on the product molecular weight 441.56. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.26 mL | 11.32 mL | 22.65 mL |
| 5 mM | 0.45 mL | 2.26 mL | 4.53 mL |
| 10 mM | 0.23 mL | 1.13 mL | 2.26 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
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Product Datasheets for Dofetilide
References for Dofetilide
References are publications that support the biological activity of the product.
Gwilt et al (1991) UK-68,798: a novel, potent and highly selective class III antiarrhythmic agent which blocks potassium channels in cardiac cells. J.Pharmacol.Exp.Ther. 256 318 PMID: 1988662
Carmeliet (1992) Voltage- and time-dependent block of delayed K+ current in cardiac myocytes by dofet. J.Pharmacol.Exp.Ther. 262 809 PMID: 1501123
Finlayson et al (2001) [3H]Dofetilide binding in SHSY5Y and HEK293 cells expressing a HERG-like K+ channel. Eur.J.Pharmacol. 412 203 PMID: 11166283
If you know of a relevant reference for Dofetilide, please let us know.
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Keywords: Dofetilide, Dofetilide supplier, UK68798, hERG, K+, potassium, channels, blockers, inhibits, IKR, delayed, rectifier, currents, Kv, voltage-gated, voltage-dependent, Human, Ether-A-Go-Go, Gene, Pfizer, KV11.1, Tikosyn, UK, 68798, Voltage-Gated, Potassium, Channels, 3757, Tocris Bioscience
5 Citations for Dofetilide
Citations are publications that use Tocris products. Selected citations for Dofetilide include:
Mark et al (2020) Reengineering an Antiarrhythmic Drug Using Patient hiPSC Cardiomyocytes to Improve Therapeutic Potential and Reduce Toxicity. Cell Stem Cell 27 813-821.e6 PMID: 32931730
McKeithan et al (2017) An Automated Platform for Assessment of Congenital and Drug-Induced Arrhythmia with hiPSC-Derived Cardiomyocytes. Front Physiol 8 766 PMID: 29075196
Carstensen et al (2019) Effects of UK 68798 and RS 43285 on atrial fibrillatory rate in a horse model of acutely induced atrial fibrillation. J Cardiovasc Electrophysiol 30 596 PMID: 30661267
Roger et al (2017) Drug delivery to the human and mouse uterus using immunoliposomes targeted to the oxytocin receptor. Am J Obstet Gynecol 216 283.e1-283.e14 PMID: 27567564
Bhave et al (2011) Development of a selective small-molecule inhibitor of Kir1.1, the renal outer medullary potassium channel. Mol Pharmacol 79 42 PMID: 20926757
Do you know of a great paper that uses Dofetilide from Tocris? Please let us know.
Reviews for Dofetilide
Average Rating: 5 (Based on 1 Review.)
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Dofetilide was used to study concentration dependent blocking action on brain Kv channels.
By
Anonymous on 10/31/2018
Assay Type: In Vitro
Species: Human
Dofetilide was used to study concentration dependent blocking action on voltage gated potassium channels on human brain cells. Dofetilide showed increasing Kv channel blocking but at high concnetrations the blocking action is hampered.
