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Propafenone/普罗帕酮 {[allProObj[0].p_purity_real_show]}

货号:A268635 同义名: SA-79

Propafenone (SA-79) 是一种钠通道阻滞剂,具有抗心律失常作用。它还对β受体具有高亲和力(IC50=32 nM)。Propafenone通过诱导线粒体功能障碍和凋亡抑制食管癌增殖。

Propafenone/普罗帕酮 化学结构 CAS号:54063-53-5
Propafenone/普罗帕酮 化学结构
CAS号:54063-53-5
Propafenone/普罗帕酮 3D分子结构
CAS号:54063-53-5
Propafenone/普罗帕酮 化学结构 CAS号:54063-53-5
Propafenone/普罗帕酮 3D分子结构 CAS号:54063-53-5
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Propafenone/普罗帕酮 纯度/质量文件 产品仅供科研

货号:A268635 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Sodium Channel 其他靶点 纯度
Tolperisone HCl 99%
Triamterene +++

ENaC, IC50: 4.5 μM

98%
Lamotrigine 98%
Vinpocetine 98%
Zonisamide 99%
Dronedarone HCl 95%
Procainamide HCl 99%
Bupivacaine HCl 99+%
Benzocaine 98%
Carbamazepine ++

Sodium channel, IC50: 131 μM

98%
Quinidine sulfate dihydrate 98%
Ibutilide fumarate 99%+
Dibucaine HCl 99+%
Mexiletine HCl 99%
Phenytoin 99+%
Camostat Mesylate +++

epithelial sodium channel (ENaC), IC50: 50 nM

99%+
Levobupivacaine 97+%
Oxcarbazepine +

sodium channel, IC50: 160 μM

98%
Amiloride HCl dihydrate 97%
Ambroxol 98+%
Primidone 99%
Propafenone 99%
A-803467 ++++

Na(V1.8) channel, IC50: 8 nM

99%+
Rufinamide 99%
Phenytoin sodium 98%
Proparacaine HCl +

Voltage-gated sodium channel, ED50: 3.4 mM

98+%
Amiloride HCl 98%
Riluzole 97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 Adrenergic Receptor α-adrenergic receptor β-adrenergic receptor 其他靶点 纯度
Ivabradine HCl 98%
Maprotiline HCl 98%
Cisatracurium besylate 96%
Yohimbine HCI 99+%
BMY 7378 ++

α2C-adrenoceptor, pKi: 6.54

α1D-adrenoceptor, pKi: 5.1

+

β1-adrenoceptor, pIC50: 5.1

97%
Asenapine maleate ++++

α2A-adrenergic receptor, pKi: 8.9

α2B-adrenergic receptor, pKi: 8.9

97%
Piribedil ++

adrenoceptor α2A, pKi: 7.1

adrenoceptor α2C, pKi: 7.2

98%
Prazosin HCl 95%
Silodosin 98%
Phenoxybenzamine HCl 98%
Labetalol HCl 98+%
Naftopidil +++

α1A-adrenergic receptor, Ki: 3.7 nM

α1D-adrenergic receptor, Ki: 20 nM

98%
Naftopidil 2HCl +

α1-adrenergic receptor, IC50: 0.2 μM

99%
Alfuzosin HCl 98%
Terazosin HCl 99%
Atipamezole 95%
Phentolamine methanesulfonate salt 99%
Carvedilol 99%
Doxazosin mesylate 99%
Tolazoline HCl 98%
Esmolol HCl 95%
Propranolol HCl ++

β-adrenergic receptor, IC50: 12 nM

99%
Zenidolol HCl ++++

β2-adrenergic receptor, Ki: 0.7nM

β1-adrenergic receptor, Ki: 611nM

98%
Acebutolol HCl 97+%
Carteolol HCl 98+%
Betaxolol 99%
Betaxolol HCl +

β1-adrenergic receptor, IC50: 6 μM

97%
Bisoprolol 97%
Sotalol HCl 95+%
Nebivolol HCl +++

β1-adrenoceptor, IC50: 0.8 nM

99%
Metoprolol 98+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 Potassium Channel 其他靶点 纯度
Tolbutamide 98%
Glimepiride ++++

SUR2B, IC50: 7.3 nM

SUR1, IC50: 5.4 nM

97%
Dronedarone HCl 95%
Gliquidone ++

Potassium channel, IC50: 27.2 nM

99%
TRAM-34 +++

IKCa1 (KCa3.1), Kd: 20 nM

98%
Glibenclamide 98%
Amiodarone HCl 97%
Gliclazide ++

Potassium channel, IC50: 184 nM

98%
Repaglinide 98%
Dofetilide 98%
Nateglinide 99%
Quinine HCl dihydrate 98%
ML133 HCl +

Kir2.1, IC50: 290 nM

99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Propafenone/普罗帕酮 生物活性

靶点
  • Sodium Channel

Propafenone/普罗帕酮 细胞实验

Cell Line
Concentration Treated Time Description References
Isolated atria 1-30 μM 45 min To assess the antagonistic effects of propafenone and diprafenone on the positive inotropic action of isoprenaline, showing that (S)-enantiomers were 14-40 times more potent than (R)-enantiomers. Br J Pharmacol. 1991 Mar;102(3):669-74.
Guinea-pig myocardial membranes 1-30 μM 30 min To determine the affinity of propafenone and diprafenone for β-adrenoceptors, showing that (S)-enantiomers were 40-60 times more potent than (R)-enantiomers. Br J Pharmacol. 1991 Mar;102(3):669-74.
SK-MEL-28 cells 5 µM 3 h Propafenone synergizes with RSL3 to induce mitochondrial-associated ferroptosis J Immunother Cancer. 2024 Nov 24;12(11):e009805.
A375 cells 5 µM 3 h Propafenone synergizes with RSL3 to induce mitochondrial-associated ferroptosis J Immunother Cancer. 2024 Nov 24;12(11):e009805.
Chinese hamster ovary cells (CHO) 5 μM To evaluate the blocking effect of propafenone on KCNA5 channels, results showed that co-expression of OCTN1 significantly enhanced the blocking effect of propafenone. Br J Pharmacol. 2010 Nov;161(5):1023-33.
MDCKII-OCTN2 100 µM 5 min To study the inhibitory effect of propafenone on OCTN2 function, results showed that propafenone had a minor effect on OCTN2 function. Am J Pathol. 2011 Jun;178(6):2547-59.
MDCKII-OCTN1 100 µM 5 min To study the inhibitory effect of propafenone on OCTN1 function, results showed that propafenone significantly inhibited OCTN1 function with an IC50 of 67.5 μM. Am J Pathol. 2011 Jun;178(6):2547-59.
MDCKII-OCT3 100 µM 90 seconds To study the inhibitory effect of propafenone on OCT3 function, results showed that propafenone significantly inhibited OCT3 function, IC50 not determined. Am J Pathol. 2011 Jun;178(6):2547-59.
MDCKII-OCT1 100 µM 5 min To study the inhibitory effect of propafenone on OCT1 function, results showed that propafenone significantly inhibited OCT1 function with an IC50 of 1.0 μM. Am J Pathol. 2011 Jun;178(6):2547-59.

Propafenone/普罗帕酮 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice SK-MEL-28 xenograft model Intraperitoneal injection 10 mg/kg Daily Combination of propafenone and RSL3 significantly suppressed tumor growth and prolonged survival J Immunother Cancer. 2024 Nov 24;12(11):e009805.
Rats Wistar rats Intracerebroventricular injection 40 μg Single injection Inhibition of brain CYP2D activity, reducing codeine-induced analgesia Biochem Pharmacol. 2013 Jun 15;85(12):1848-55

Propafenone/普罗帕酮 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.93mL

0.59mL

0.29mL

14.64mL

2.93mL

1.46mL

29.29mL

5.86mL

2.93mL

Propafenone/普罗帕酮 技术信息

CAS号54063-53-5
分子式C21H27NO3
分子量 341.44
SMILES Code O=C(C1=CC=CC=C1OCC(O)CNCCC)CCC2=CC=CC=C2
MDL No. MFCD00216020
别名 SA-79
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

DMSO: 120 mg/mL(351.45 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

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