Propafenone
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.96%
- CAS 番号: 54063-53-5
- 分子式: C21H27NO3
- 分子量:341.44
-
保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Propafenone
MoreAdrenergic Receptor アイソフォーム固有の製品をすべて表示
More
生物活性
|
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] |
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 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.
-
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 54063-53-5
-
性状 Solid
-
分子量 341.44
-
分子式 C21H27NO3
-
Color White to off-white
-
SMILES
O=C(C1=CC=CC=C1OCC(O)CNCCC)CCC2=CC=CC=C2
-
別名
SA-79
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
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
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (277 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
取扱説明書 (2659 KB)
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. [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
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 |
Propafenone 関連分類
HY-B0432 関連分類
Powered by Bioz