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Selective potassium channel blocker. Blocks KV11.1 (hERG) channels; inhibits the rapid delayed-rectifier K+ current (IKr). Displays class III antiarrhythmic properties.
Sold for research purposes under agreement from Pfizer Inc.
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
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|
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
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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
3 Citations for Dofetilide
Citations are publications that use Tocris products. Selected citations for Dofetilide include:
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
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
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Reviews for Dofetilide
Average Rating: 5 (Based on 1 Review.)
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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.
Literature in this Area
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Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.