Propafenone HCl is a sodium-channel blocker that also has a high affinity for β-receptors (IC50 = 32 nM). It blocks transient outward potassium current (Ito) and sustained delayed rectifier K+ current (Isus) with IC50 values of 4.9 μM and 8.6 μM, respectively.In addition, Propafenone inhibits the proliferation of esophageal cancer by inducing mitochondrial dysfunction and apoptosis.
| Molecular Weight | 377.9 |
| Formula | C21H27NO3.HCl |
| CAS Number | 34183-22-7 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] L L Dupuis, et al. Stability of propafenone hydrochloride in i.v. solutions
[3] C Funck-Brentano, et al. Propafenone
[4] D Veale, et al. Propafenone
[5] J T Hii, et al. Clinical pharmacokinetics of propafenone
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Psalmotoxin 1 (PcTx1) is a protein toxin that can bind at subunit-subunit interfaces of acid-sensing ion channel 1a (ASIC1a). |
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Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms. |
| Huwentoxin-IV
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