Sildenafil citrate is an agent used to treat erectile dysfunction and pulmonary arterial hypertension (PAH). Sildenafil citrate acts by inhibiting cGMP specific phosphodiesterase type 5, an enzyme that regulates blood flow in the penis. Sildenafil has been the prime treatment for erectile dysfunction.
| Molecular Weight | 666.7 |
| Formula | C22H30N6O4S.C6H8O7 |
| CAS Number | 171599-83-0 |
| Solubility (25°C) | DMSO 50 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.
[1] Sukhdeep Bhogal, et al. Sildenafil for Pulmonary Arterial Hypertension
[2] Pramod Krishnappa, et al. Sildenafil/Viagra in the treatment of premature ejaculation
[4] S Graziano, et al. Sildenafil-associated hepatoxicity: a review of the literature
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