Propafenone(Synonyms: SA-79)

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Propafenone (Synonyms: SA-79)

Propafenone (SA-79) 是一种钠通道 (sodium-channel) 阻滞剂，具有抗心律失常的作用。Propafenone 对 β 受体也具有高亲和力 (IC50=32 nM)。Propafenone 阻断瞬时外向钾电流 (Ito) 和持续延迟整流器 K+ 电流 (Isus)，IC50 值分别为 4.9 μM 和 8.6 μM。Propafenone 通过诱导线粒体功能障碍和诱导细胞凋亡 (apoptosis) 抑制食管癌增殖。

Propafenone(Synonyms: SA-79)

Propafenone Chemical Structure

CAS No. : 54063-53-5

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Propafenone 的其他形式现货产品:

Propafenone hydrochloride (S)-Propafenone

生物活性

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].

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd 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.

体内研究
(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].

Shanghai Jinpan Biotech Co Ltd 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.

分子量

341.44

Formula

C21H27NO3
CAS 号

54063-53-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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

  • [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.

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

    [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.

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