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In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Dofetilide is a potassium channel blocker.
Cell lines
HEK293 cells, guinea pig cardiomyocytes
Preparation method
The solubility of this compound in DMSO is >21.2 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reacting condition
1 μM
Applications
In a human cell line and human embryonic kidney 293 transfected with HERG, dofetilide induced channel block with the EC50 of 12 ± 2 nM. Induction of block depended on depolarization beyond the threshold for channel opening. Dofetilide acted as a slow-onset/slow-offset open channel blocker of this current at nanomolar concentrations. Dofetilide (1 μM) reduced the amplitude of IKr to 61% of control currents in guinea pig cardiomyocytes, as measured by 200-ms test pulses and analysis of the deactivating tail currents of IKr.
Animal models
Dogs with old myocardial infarction (MI)
Dosage form
Intravenous injection, 100 mg/kg
Application
Dofetilide (100 mg/kg, i.v.) suppressed the reentry arrhythmia induced by PES in dogs with old myocardial infarction (MI). Dofetilide showed antiarrhythmic effect in some dogs with digitalis arrhythmia. Dofetilide increased QT interval and showed negative chronotropic effect.
Other notes
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References:
[1]. Snyders D J, Chaudhary A. High affinity open channel block by dofetilide of HERG expressed in a human cell line[J]. Molecular Pharmacology, 1996, 49(6): 949-955.
[2]. Kiehn J, Villena P, Beyer T, et al. Differential effects of the new class III agent dofetilide on potassium currents in guinea pig cardiomyocytes[J]. Journal of cardiovascular pharmacology, 1994, 24(4): 566-572.
[3]. Chen J, Xue Y, Eto K, et al. Effects of dofetilide, a class III antiarrhythmic drug, on various ventricular arrhythmias in dogs[J]. Journal of cardiovascular pharmacology, 1996, 28(4): 576-584.
