1. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein
  2. Sodium Channel Adrenergic Receptor Potassium Channel
  3. Propafenone

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

Propafenone Chemical Structure

CAS No. : 54063-53-5

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Based on 1 publication(s) in Google Scholar

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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].

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.
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
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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Purity & Documentation
References

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.

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
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Help & FAQs
  • Do most proteins show cross-species activity?

    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
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