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

Propafenone (SA-79) 是一種鈉通道 (sodium-channel) 阻滯劑，具有抗心律失常的作用。Propafenone 對 β 受體也具有高親和力 (IC50=32 nM)。Propafenone 阻斷瞬時外向鉀電流 (Ito) 和持續(xù)延遲整流器 K+ 電流 (Isus)，IC50 值分別為 4.9 μM 和 8.6 μM。Propafenone 通過誘導(dǎo)線粒體功能障礙和誘導(dǎo)細(xì)胞凋亡 (apoptosis) 抑制食管癌增殖。

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Propafenone Chemical Structure

Propafenone Chemical Structure

CAS No. : 54063-53-5

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥550
In-stock
25 mg ￥500
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50 mg ￥800
In-stock
100 mg ￥1300
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200 mg   詢價  
500 mg   詢價  

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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

查看 Sodium Channel 亞型特異性產(chǎn)品:

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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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].

細(xì)胞效力
(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]
體外研究
(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].

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.
體內(nèi)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].

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
分子量

341.44

Formula

C21H27NO3
CAS 號
性狀

固體

顏色

White to off-white

運輸條件

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

4°C, protect from light

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

溶解性數(shù)據(jù)
細(xì)胞實驗： 

DMSO 中的溶解度 : 125 mg/mL (366.10 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.93%

參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 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
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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Inquiry Information

產(chǎn)品名稱：
Propafenone
目錄號：
HY-B0432
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