Felodipine is widely used to study angina and hypertension. The IC50 of felodipine was ~8 nM, which was about 50 times higher than nifedipine and 430 times higher than verapamil in KCL contractile pig coronary artery segment by blocking Ca2+ channel. Filodipine significantly induced transcription and secretion of IL-6 and IL-8 in human VSMC and lung fibroblasts with ED50 values of 5.8 nM and 5.3 nM, respectively, while propranolol and furosemide did not affect the expression of these two IL-6 genes. Felodipine can block Ca2+ dependent contraction of rat ileum longitudinal smooth muscle (GPILSM) with IC50 of 1.45 nM.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Male Sprague-Dawley rats with approximately 5/6 renal ablation |
| Formulation | Dissolved in DMSO, and diluted in saline |
| Dosages | 1 g/kg/day |
| Administration | Orally |
| Molecular Weight | 384.25 |
| Formula | C18H19Cl2NO4 |
| CAS Number | 72509-76-3 |
| Form | Solid |
| Solubility (25°C) | DMSO 47 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.
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