Propafenone (Synonyms: SA-79)

Name: Propafenone
Brand: MedChemExpress
SKU: HY-B0432
Rating: 4.5 (1 reviews)

Cat. No.: HY-B0432 Purity: 99.93%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Propafenone Chemical Structure

CAS No. : 54063-53-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
25 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 130	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Propafenone:

1 Publications Citing Use of MCE Propafenone

•Bioorg Chem. 2024 Apr 29:147:107412. [Abstract]

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Na_v1.1 Na_v1.2 Na_v1.3 Na_v1.4 Na_v1.5 Na_v1.6 Na_v1.7 Na_v1.8

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α adrenergic receptor β adrenergic receptor

Biological Activity
Purity & Documentation
References
Customer Review

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].

Cellular Effect

Cell Line	Type	Value	Description	References
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	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]
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]
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	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]
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]
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	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]
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]

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.

Clinical Trial

Molecular Weight

341.44

Formula

C₂₁H₂₇NO₃

CAS No.

54063-53-5

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Concentration _(final)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.93%

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Data Sheet (276 KB) SDS (251 KB)

COA (250 KB) HNMR (279 KB) LCMS (87 KB)

Handling Instructions (2659 KB)

References

[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]

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 Related Classifications

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Propafenone (Synonyms: SA-79)

Customer Review

Other Forms of Propafenone:

Propafenone Related Antibodies

1 Publications Citing Use of MCE Propafenone

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Propafenone Related Antibodies

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Complete Stock Solution Preparation Table

Propafenone Related Classifications

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