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Cat. No. Name Size Price Add Cart
KI0777Dofetilide10 mg$154
Dofetilide50 mg$496

Chemical Characteristic

Product NameDofetilide
SynonymsTikosyn
CAS No.115256-11-6
Molecular Weight 441.56
FormulaC19H27N3O5S2
Chemical NameN-[4-(2-{2-[4-(methanesulphonamido)phenoxyl]-N-methylethylamino}ethyl)phenyl]-methanesulphonamide
SmilesCS(=O)(=O)Nc1ccc(cc1)CCN(CCOc1ccc(cc1)NS(=O)(=O)C)C
Chemical Structure

Biological activities

Dofetilide is a standard class III antiarrhythmic agent. Dofetilide is used for the management of atrial fibrillation (AF) and is effective in the treatment of a range of cardiac arrhythmias. Dofetilide potently blocks rectifier K+ current (IKr). The IC50 of dofetilide for HERG1 A and S620T is 0.32 and 248 µM, respectively. Dofetilide inhibits BEAG T432S and BEAG WT with IC50 of 1.0 and 32.0µM, respectively. Dofetilide also inhibits the S631A mutation and the S631A/F656V double mutation with IC50 of 20.0 and 32.0µM, respectively.[1] Dofetilide interaction with HERG channels expressed in Xenopus oocytes requires membrane depolarization.[2] In vivo in anesthetized dogs, dofetilide at 10µg/kg per minute significantly increases LVSP and maximum left-ventricular developed pressure-increase rate and decreases heart rate. Dofetilide also significantly prolongs QT and QTc intervals.[3]

Protocols

Dofetilide is diluted in DMSO.[1]

References

[1] Lees-Miller JP, et al. Molecular determinant of high-affinity dofetilide binding to HERG1 expressed in Xenopus oocytes: involvement of S6 sites. Mol Pharmacol. 2000, 57 (2): 367-374.
[2] Weerapura M, et al. Dofetilide block involves interactions with open and inactivated states of HERG channels. Pflugers Arch. 2002, 443(4): 520-531.
[3] Hashimoto N, et al. Characterization of in vivo and in vitro electrophysiological and antiarrhythmic effects of a novel IKACh blocker, NIP-151: a comparison with an IKr-blocker dofetilide. J Cardiovasc Pharmacol. 2008, 51(2): 162-169.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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