product name Sildenafil Citrate
Description: Sildenafil Citrate, a potent and selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5), is a well-tolerated and highly effective treatment for erectile dysfunction. Sildenafil, Citrate is a citrate form of Sildenafil. As a PDE5 inhibitor, Sildenafil has been reported to enhance neuro-, synapto- and angiogenesis in rat models of stroke and also is reported to be a mild vasodilator. Sildenafil has also been shown to prevent indomethacin-induced small intestinal ulceration formation through an NO/cGMP- dependent mechanism.
References: World J Urol. 2001 Feb;19(1):40-5.
666.7
Formula
C22H30N6O4S.C6H8O7
CAS No.
171599-83-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 20 mg/mL (30.0 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Sildenafil citrate is a potent PDE type 5 reversible and selective inhibitor that blocks cGMP hydrolysis effectively (Ki ∼3 nM). Sildenafil exhibited high affinity for PDE type 5 and type 6 with inhibition constants (Ki) of ∼3.5 and 33 nM, respectively. Sildenafil enhances sodium nitroprusside- or transmural electrical stimulation-induced relaxation of precontracted corpus cavernosum muscle strips in organ baths, suggesting that sildenafil augments the activity of NO-mediated relaxation. Sildenafil citrate increases intracellular cGMP concentrations in cultured smooth muscle cells treated with sodium nitroprusside and in rabbit corpus cavernosum in vitro. Sildenafil is metabolized in the liver by cytochrome P450 and is converted into an active metabolite with characteristics similar to the parent compound. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Sildenafil citrate enhances erectile function following pelvic nerve stimulation in anesthetized dogs as measured by increased intracavernosal pressure. Sildenafil citrate significantly reverses impaired carbachol-stimulated relaxation and inhibits superoxide formation by cavernosal tissue from hypercholesterolaemic rabbits. Sildenafil improves erectile function in a time- and dose-dependent fashion with maximization of erectile function recovery occurring with daily 20 mg/kg at the 28-day time point in Sprague-Dawley rats. Sildenafil use results in smooth muscle-collagen ratio protection and CD31 and eNOS expression preservation in Sprague-Dawley rats. Sildenafil reduces apoptotic indices significantly compared with control, and increases phosphorylation of akt and eNOS in Sprague-Dawley rats. |
| Animal model | Sprague-Dawley rats |
| Formulation & Dosage | 20 mg/kg |
| References | Eur J Pharmacol. 2005 Jul 11;517(3):224-31; J Sex Med. 2008 May;5(5):1126-36. |
