Clofilium phosphate  (Synonyms: LY 150378)

Clofilium phosphate (LY 150378) is an antiarrhythmic/antifibrillatory agent. Clofilium phosphate significantly prolongs the action potential duration and effective refractory period of canine cardiac Purkinje fibers, increases the ventricular fibrillation threshold, reduces the risk of reentrant arrhythmias, and enables spontaneous conversion of some ventricular fibrillation episodes to sinus rhythm. Clofilium phosphate is applicable to research related to ventricular fibrillation, arrhythmias, and ventricular tachyarrhythmias^[1][2][3].

Clofilium phosphate selectively prolongs the action potential duration and effective refractory period of Purkinje fibers in normal dogs^[1].
Clofilium phosphate (30-100 nM) prolongs the action potential duration of canine papillary muscle and ventricular free wall cells, but exerts no effect on the APD of atrial muscle at the tested concentrations^[1].
Clofilium phosphate (30-1000 nM; for at least 1 h) selectively prolongs the action potential duration and refractory period of isolated normal canine Purkinje fibers, without significantly altering membrane responsiveness, conduction velocity, or diastolic depolarization rate; its APD-prolonging effect is more pronounced under conditions of longer basic cycle lengths and in depolarized fibers at higher concentrations^[2].
Clofilium phosphate (0.01-10 μM; 30 min) potently prolongs the APD₉₅ of isolated canine cardiac Purkinje fibers, with a C₂₀APD₉₅ value of 0.26 μM, and produces a maximum 39 ± 8% increase in APD₉₅ at 10 μM^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clofilium phosphate (0.5-1.0 µmole/kg; intravenous injection; 30 min infusion) dose-dependently increases the ventricular fibrillation threshold in anesthetized mongrel dogs^[1].
Clofilium phosphate (10 mg/kg; intradermal injection) prolongs the left ventricular functional refractory period of anesthetized healthy mongrel dogs by at least 12%^[3].
Clofilium phosphate (0.1-10 mg/kg; intravenous injection) prevents programmed electrical stimulation-induced ventricular tachycardia in 70% of anesthetized mongrel dogs with 24-hour-old myocardial infarction^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

435.97

C₂₁H₃₉ClNO₄P

68379-03-3

O=P([O-])(O)O.ClC1=CC=C(C=C1)CCCC[N+](CC)(CC)CCCCCCC

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Steinberg M I, et al. Clofilium1--a new antifibrillatory agent that selectively increases cellular refractoriness. Life Sciences, 1979, 25(16): 1397-1406.

  [2]. Steinberg MI, et al. Cellular electrophysiology of clofilium, a new antifibrillatory agent, in normal and ischemic canine Purkinje fibers. J Cardiovasc Pharmacol. 1981;3(4):881-895.  [Content Brief]

  [3]. Lis R, et al. Synthesis and antiarrhythmic activity of novel 3-alkyl-1-[omega-[4-[(alkylsulfonyl)amino]phenyl]-omega- hydroxyalkyl]-1H-imidazolium salts and related compounds. J Med Chem. 1987 Apr;30(4):696-704.  [Content Brief]