Cat. No.: HY-B0432

Propafenone

(Synonyms: SA-79)

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

Propafenone (SA-79), a sodium-channel blocker, acts an antiarrhythmic agent. Propafenone also has high affinity for the β receptor (IC₅₀=32 nM). Propafenone blocks the transient outward current (Ito) and the sustained delayed rectifier K current (Isus) with IC₅₀ values of 4.9 μm and 8.6 μm, respectively. Propafenone suppresses esophageal cancer proliferation through inducing mitochondrial dysfunction and induce apoptosis.

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Pureté: 99.96%
CAS No.: 54063-53-5
Formule: C₂₁H₂₇NO₃
Masse moléculaire:341.44

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4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Propafenone Chemical Structure

CAS No.: 54063-53-5

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (2)
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Propafenone (SA-79), a sodium-channel blocker, acts an antiarrhythmic agent. Propafenone also has high affinity for the β receptor (IC₅₀=32 nM)^[1]. Propafenone blocks the transient outward current (Ito) and the sustained delayed rectifier K current (Isus) with IC₅₀ values of 4.9 μm and 8.6 μm, respectively^[2]. Propafenone suppresses esophageal cancer proliferation through inducing mitochondrial dysfunction and induce apoptosis^[3].

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Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	ED₅₀	88 nM Compound: 1 (Propafenone)	The chemosensitizing effect was measured against P-glycoprotein expressing CCRF-CEM cells in the presence of 5 uM daunomycin The chemosensitizing effect was measured against P-glycoprotein expressing CCRF-CEM cells in the presence of 5 uM daunomycin	[PMID: 7629817]
CCRF-CEM	ED₅₀	0.29 μM Compound: 1a	Effective dose against CCRF-CEM vcr 100 cells by using MTT assay Effective dose against CCRF-CEM vcr 100 cells by using MTT assay	[PMID: 8941391]
CCRF-CEM	ED₅₀	0.29 μM/L Compound: 1a	Effective dose against CCRF-CEM vcr 100 cells by using MTT assay Effective dose against CCRF-CEM vcr 100 cells by using MTT assay	[PMID: 8941391]
CCRF-CEM	ED₅₀	3.55 μM Compound: 1a	Effective dose against CCRF-CEM vcr 100 cells by using rhodamine efflux studies. Effective dose against CCRF-CEM vcr 100 cells by using rhodamine efflux studies.	[PMID: 8941391]
CCRF-CEM	ED₅₀	3.55 μM/L Compound: 1a	Effective dose against CCRF-CEM vcr 100 cells by using rhodamine efflux studies. Effective dose against CCRF-CEM vcr 100 cells by using rhodamine efflux studies.	[PMID: 8941391]
CCRF-CEM	EC₅₀	0.32 μM Compound: propafenone	Compound was tested for inhibition of daunomycin efflux in the resistant human T-lymphoblast cell line CEM vcr1000. Compound was tested for inhibition of daunomycin efflux in the resistant human T-lymphoblast cell line CEM vcr1000.	[PMID: 9767638]
CCRF-CEM/VCR-1000	IC₅₀	1.08 μM Compound: 1	In vitro multi drug resistance (MDR) reversal inhibitory activity against CCRF-CEM/VCR-1000 cell line In vitro multi drug resistance (MDR) reversal inhibitory activity against CCRF-CEM/VCR-1000 cell line	[PMID: 14584949]
CHO	IC₅₀	>5 μM Compound: Propafenone	Inhibition of human cloned Nav1.5 channel expressed in chinese hamster CHO cells assessed as phasic inhibition after 5 mins by patch clamp assay Inhibition of human cloned Nav1.5 channel expressed in chinese hamster CHO cells assessed as phasic inhibition after 5 mins by patch clamp assay	[PMID: 21955244]
CHO	IC₅₀	2.88 μM Compound: Propafenone	Inhibition of human cloned ERG channel expressed in chinese hamster CHO cells after 5 mins by patch clamp assay Inhibition of human cloned ERG channel expressed in chinese hamster CHO cells after 5 mins by patch clamp assay	[PMID: 21955244]
CHO	IC₅₀	3.3 μM Compound: Propafenone	Inhibition of human cloned Nav1.5 channel expressed in chinese hamster CHO cells assessed as tonic inhibition after 5 mins by patch clamp assay Inhibition of human cloned Nav1.5 channel expressed in chinese hamster CHO cells assessed as tonic inhibition after 5 mins by patch clamp assay	[PMID: 21955244]
CHO	IC₅₀	5.1 μM Compound: 37	Inhibition of of TASK1 (unknown origin) expressed in CHO cells assessed as reduction in channel currents Inhibition of of TASK1 (unknown origin) expressed in CHO cells assessed as reduction in channel currents	[PMID: 26588045]
CHO	IC₅₀	7.6 μM Compound: 37	Inhibition of of human TREK1 expressed in CHO cells assessed as reduction in channel currents Inhibition of of human TREK1 expressed in CHO cells assessed as reduction in channel currents	[PMID: 26588045]
HEK293	IC₅₀	11.1 μM Compound: propafenone	Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy	[PMID: 18788725]
HEK293	IC₅₀	1190 nM Compound: Propafenone	Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA	[PMID: 21300721]
HEK293	IC₅₀	2.2 μM Compound: Propafenone	Inhibition of human kir6.2/SUR2A ion channel coexpressed in human HEK293 cells after 5 mins by patch clamp assay Inhibition of human kir6.2/SUR2A ion channel coexpressed in human HEK293 cells after 5 mins by patch clamp assay	[PMID: 21955244]
HEK293	IC₅₀	15.54 μM Compound: Propafenone	Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay	[PMID: 28230985]
Huh-7	CC₅₀	28.86 μM Compound: GNF-Pf-4594	NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7) NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)	[PMID: 18579783]
L02	IC₅₀	48.2 μM Compound: PPF	Antiproliferative activity against human HL7702 cells cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay Antiproliferative activity against human HL7702 cells cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay	[PMID: 36868105]
MDR	EC₅₀	0.329 μM Compound: 22	Inhibition of P-glycoprotein expressed in MDR CCRF vcr1000 cells by daunorubicin efflux assay Inhibition of P-glycoprotein expressed in MDR CCRF vcr1000 cells by daunorubicin efflux assay	[PMID: 17352460]
Ventricular myocyte	IC₅₀	1800 nM Compound: Propafenone	Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes	[PMID: 21300721]
Ventricular myocyte	IC₅₀	1.8 μM Compound: Propafenone	Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes	[PMID: 22761000]

In Vitro

Propafenone (5-25 μM) inhibits esophageal squamous cell carcinoma (ESCC) cell proliferation^[3].
Propafenone causes mitochondrial dysfunction by a decreased mitochondrial membrane potential and reduced expression of Bcl-xL and Bcl-2^[3].
Propafenone (10 and 20 μm) treatment significantly down regulates the expression levels of the anti-apoptotic proteins Bcl-xL and Bcl-2 in ESCC cells. Propafenone also reduces expression of p-ERK^[3].

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

Cell Proliferation Assay^[3]

Cell Line:

The human ESCC cell lines KYSE30, KYSE150 and KYSE270
Concentration:

5, 10, 15, 20, and 25 μm
Incubation Time:

24, 48, and 72 hours
Result:

Gradually decreased cell proliferation over time and potently inhibited cell proliferation with increasing concentrations in KYSE30, KYSE150 and KYSE270 cells.

Western Blot Analysis^[3]

Cell Line:

The human ESCC cell lines KYSE30, KYSE150 and KYSE270
Concentration:

0, 10, and 20 μm
Incubation Time:

72 hours
Result:

Significant downregulation of Bcl-xL and Bcl-2 expression levels was observed.

In Vivo

Propafenone (20 mg/kg; intraperitoneal injection every other day) markedly suppresses the tumor burden with a decrease of 69.2%^[3].
Propafenone also significantly inhibits tumor cell proliferation (mean index decreased from 56.3±6.7% in the DMSO-treated group to 20.7±5.1% in the 10 mg/kg propafenone-treated group and 11.3±4.0% in the 20 mg/kg propafenone-treated group)^[3].

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

Animal Model:

Female BALB/c nude mice bearing KYSE270-derived xenografts (6-8 weeks)^[3]
Dosage:

10 mg/kg or 20 mg/kg
Administration:

Intraperitoneally injected
Result:

Exerted a significantly inhibitory effect on the growth of tumor xenografts.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 54063-53-5
Appearance Solid
Masse moléculaire 341.44
Formule C₂₁H₂₇NO₃
Color White to off-white
SMILES

O=C(C1=CC=CC=C1OCC(O)CNCCC)CCC2=CC=CC=C2
Synonyms

SA-79
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (2)

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Environ Sci Technol

Data-Driven Discovery of Unknown Precursors of N-Nitrosodimethylamine in Nontargeted Liquid Chromatography-High Resolution Mass Spectrometry Analysis. [Abstract]

2026 Mar 3;60(8):6558-6568. PMID: 41714108
Bioorg Chem

Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]

2024 Jun:147:107412. PMID: 38696845

Solvant et solubilité

In Vitro:

DMSO : 125 mg/mL (366.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9288 mL

14.6439 mL

29.2877 mL

5 mM

0.5858 mL

2.9288 mL

5.8575 mL

10 mM

0.2929 mL

1.4644 mL

2.9288 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
SDS (393 KB)
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- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. J T Lee, et al. The role of genetically determined polymorphic drug metabolism in the beta-blockade produced by propafenone. N Engl J Med. 1990 Jun 21;322(25):1764-8. [Content Brief]

[2]. A Seki, et al. Effects of propafenone on K currents in human atrial myocytes. Br J Pharmacol. 1999 Mar;126(5):1153-62. [Content Brief]

[3]. Wei-Bin Zheng, et al. Propafenone suppresses esophageal cancer proliferation through inducing mitochondrial dysfunction. Am J Cancer Res. 2017 Nov 1;7(11):2245-2256. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.9288 mL	14.6439 mL	29.2877 mL	73.2193 mL
	5 mM	0.5858 mL	2.9288 mL	5.8575 mL	14.6439 mL
	10 mM	0.2929 mL	1.4644 mL	2.9288 mL	7.3219 mL
	15 mM	0.1953 mL	0.9763 mL	1.9525 mL	4.8813 mL
	20 mM	0.1464 mL	0.7322 mL	1.4644 mL	3.6610 mL
	25 mM	0.1172 mL	0.5858 mL	1.1715 mL	2.9288 mL
	30 mM	0.0976 mL	0.4881 mL	0.9763 mL	2.4406 mL
	40 mM	0.0732 mL	0.3661 mL	0.7322 mL	1.8305 mL
	50 mM	0.0586 mL	0.2929 mL	0.5858 mL	1.4644 mL
	60 mM	0.0488 mL	0.2441 mL	0.4881 mL	1.2203 mL
	80 mM	0.0366 mL	0.1830 mL	0.3661 mL	0.9152 mL
	100 mM	0.0293 mL	0.1464 mL	0.2929 mL	0.7322 mL

Propafenone

2 Cited Publications

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Propafenone

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Publications Citing Use of MedChemExpress (MCE) Propafenone

Voir tous les produits spécifiques à Isoform Sodium Channel

Voir tous les produits spécifiques à Isoform Adrenergic Receptor

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Propafenone Related Classifications

HY-B0432 Related Classifications