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Chemical Structure| 54063-53-5 Chemical Structure| 54063-53-5

Structure of Propafenone
CAS No.: 54063-53-5

Chemical Structure| 54063-53-5

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Propafenone (SA-79) is a sodium channel blocker with antiarrhythmic effects. It also has high affinity for β receptors (IC50=32 nM). Propafenone inhibits esophageal cancer proliferation by inducing mitochondrial dysfunction and apoptosis.

Synonyms: SA-79

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Product Details of Propafenone

CAS No. :54063-53-5
Formula : C21H27NO3
M.W : 341.44
SMILES Code : O=C(C1=CC=CC=C1OCC(O)CNCCC)CCC2=CC=CC=C2
Synonyms :
SA-79
MDL No. :MFCD00216020

Safety of Propafenone

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P264-P270-P301+P312-P330-P501

Related Pathways of Propafenone

GPCR

Isoform Comparison

Biological Activity

Target
  • Sodium Channel

In Vitro:

Cell Line
Concentration Treated Time Description References
Isolated atria 1-30 μM 45 min To assess the antagonistic effects of propafenone and diprafenone on the positive inotropic action of isoprenaline, showing that (S)-enantiomers were 14-40 times more potent than (R)-enantiomers. Br J Pharmacol. 1991 Mar;102(3):669-74.
Guinea-pig myocardial membranes 1-30 μM 30 min To determine the affinity of propafenone and diprafenone for β-adrenoceptors, showing that (S)-enantiomers were 40-60 times more potent than (R)-enantiomers. Br J Pharmacol. 1991 Mar;102(3):669-74.
SK-MEL-28 cells 5 µM 3 h Propafenone synergizes with RSL3 to induce mitochondrial-associated ferroptosis J Immunother Cancer. 2024 Nov 24;12(11):e009805.
A375 cells 5 µM 3 h Propafenone synergizes with RSL3 to induce mitochondrial-associated ferroptosis J Immunother Cancer. 2024 Nov 24;12(11):e009805.
Chinese hamster ovary cells (CHO) 5 μM To evaluate the blocking effect of propafenone on KCNA5 channels, results showed that co-expression of OCTN1 significantly enhanced the blocking effect of propafenone. Br J Pharmacol. 2010 Nov;161(5):1023-33.
MDCKII-OCTN2 100 µM 5 min To study the inhibitory effect of propafenone on OCTN2 function, results showed that propafenone had a minor effect on OCTN2 function. Am J Pathol. 2011 Jun;178(6):2547-59.
MDCKII-OCTN1 100 µM 5 min To study the inhibitory effect of propafenone on OCTN1 function, results showed that propafenone significantly inhibited OCTN1 function with an IC50 of 67.5 μM. Am J Pathol. 2011 Jun;178(6):2547-59.
MDCKII-OCT3 100 µM 90 seconds To study the inhibitory effect of propafenone on OCT3 function, results showed that propafenone significantly inhibited OCT3 function, IC50 not determined. Am J Pathol. 2011 Jun;178(6):2547-59.
MDCKII-OCT1 100 µM 5 min To study the inhibitory effect of propafenone on OCT1 function, results showed that propafenone significantly inhibited OCT1 function with an IC50 of 1.0 μM. Am J Pathol. 2011 Jun;178(6):2547-59.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice SK-MEL-28 xenograft model Intraperitoneal injection 10 mg/kg Daily Combination of propafenone and RSL3 significantly suppressed tumor growth and prolonged survival J Immunother Cancer. 2024 Nov 24;12(11):e009805.
Rats Wistar rats Intracerebroventricular injection 40 μg Single injection Inhibition of brain CYP2D activity, reducing codeine-induced analgesia Biochem Pharmacol. 2013 Jun 15;85(12):1848-55

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03674658 Atrial Fibrillation COMPLETED 2021-08-17 Kaohsiung Medical University C... More >>hung-Ho Memorial Hospital, Kaohsiung, Taiwan Less <<
NCT01956487 Arrhythmia, Cardiac PHASE1 COMPLETED 2012-06-27 GSK Investigational Site, Balt... More >>imore, Maryland, 21225, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.93mL

0.59mL

0.29mL

14.64mL

2.93mL

1.46mL

29.29mL

5.86mL

2.93mL

 

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