Molecular Formula | C28H38N6O11S |
Molar Mass | 666.7 |
Density | 1.447g/cm3 |
Melting Point | 187-189°C |
Boling Point | 698.72°C at 760 mmHg |
Flash Point | 376.372°C |
Water Solubility | 3.488g/L(temperature not stated) |
Solubility | DMSO: >20mg/mL |
Vapor Presure | 0mmHg at 25°C |
Appearance | white powder |
Color | White |
Merck | 14,8489 |
Storage Condition | 2-8°C |
Stability | Store in Freezer |
Refractive Index | 1.683 |
Physical and Chemical Properties | Appearance: white crystalline powder solubility: soluble in dimethylformamide Melting Point: 190-193 |
In vitro study | Sildenafil citrate is a potent reversible selective inhibitor of PDE Ⅴ, which can effectively block the hydrolysis of cGMP (Ki ∼ 3 nM). Sildenafil exhibited high affinity for type PDE Ⅴ and Ⅵ with inhibition constants (Ki) of ∼ 3.5 and 33 nM, respectively. In the organ bath, Sildenafil enhanced the relaxation of precontracted corpus cavernosum smooth muscle induced by sodium nitropramizate or transmural electrical stimulation, suggesting that sildenafil enhanced NO-mediated diastolic activity. Sildenafil citrate increased intracellular cGMP concentrations in cultured sodium nitroprunate-treated smooth muscle cells and in rabbit corpus cavernosum in vitro. In the liver, Sildenafil is metabolized by cytochrome P450 and converted into an active metabolite with properties similar to the parent compound. |
In vivo study | In anesthetized dogs, Sildenafil citrate enhances penile erectile function under pelvic nerve stimulation by measuring intracavernous pressure. Sildenafil citrate significantly reversed the impaired Carbachol-stimulated relaxation and inhibited the formation of superoxide in the corpus cavernosum tissue of hypercholesterolemic rabbits. In Sprague-Dawley rats, Sildenafil improved erectile function in a time-dose-dependent manner, with maximal erectile recovery occurring on day 28 at a dose of 20 mg/kg daily. In Sprague-Dawley rats, the use of Sildenafil resulted in preservation of smooth muscle collagen ratio and preservation of CD31 and eNOS expression. In Sprague-Dawley rats, Sildenafil significantly reduced the apoptotic index and increased the phosphorylation of akt and eNOS compared to controls. |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | 36 - Wear suitable protective clothing. |
WGK Germany | 3 |
RTECS | TL4284390 |
HS Code | 2933595960 |