Tadalafil (Cialis) is a PDE inhibitor. Tadalafil (Cialis), which has demonstrated a high level of selectivity for PDE5 over the other phosphodiesterases, has shown efficacy in improving erectile function and sexual satisfaction in phase III trials. PDE11A3, PDE11A2, and PDE11A1, which contain progressively shorter N-termini, were more sensitive than PDE11A4 to inhibition by Tadalafil (Cialis).
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Sham-operated rats |
| Formulation | Saline |
| Dosages | 2 mg/kg |
| Administration | Orally |
| Molecular Weight | 389.4 |
| Formula | C22H19N3O4 |
| CAS Number | 171596-29-5 |
| Solubility (25°C) | DMSO 48 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.
[3] Fabiola Zakia Mnica, et al. Tadalafil for the treatment of benign prostatic hyperplasia
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