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。


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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。 | |||||||||||||||||||
| 靶点 |
|
| 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. |
| 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 |
| 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 |
|
| 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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