|Sildenafil mesylate PDE5 inhibitor|
Sample solution is provided at 25 µL, 10mM.
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|Cas No.||131543-23-2||SDF||Download SDF|
|Chemical Name||5-(2-ethoxy-5-((4-methylpiperazin-1-yl)sulfonyl)phenyl)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one methanesulfonate|
|Solubility||>57.1mg/mL in DMSO||Storage||Store at -20°C|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
IC50: 3.5 nM
Sildenafil mesylate is an inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5).
PDE5 is the predominant phosphodiesterase in the corpus cavernosum. The catalytic site of PDE5 degrades cGMP, and PDE5 inhibitors can potentiate endogenous increases in cGMP.
In vitro: Sildenafil mesylate had been identified as a potent PDE5 reversible and selective inhibitor. Sildenafil enhanced sodium nitroprusside- or transmural electrical stimulation-induced relaxation of precontracted corpus cavernosum muscle strips in organ baths. Sildenafil also increased intracellular cGMP concentrations in cultured smooth muscle cells treated with sodium nitroprusside .
In vivo: In anesthetized dogs, sildenafil could enhance the erectile function following pelvic nerve stimulation as measured by increased intracavernosal pressure .
Clinical trial: Ten previous randomised controlled trials had been conducted. Dose optimisation resulted in >60% of attempts at sexual intercourse, which was successful in 49% of men. Sildenafil treatment related adverse events occurred in 30% of men compared with 11% on placebo. Dose optimisation of sildenafil showed efficacy equivalent to the highest fixed doses, and adverse events equivalent to the lowest fixed doses .
 Nehra A,Colreavy F,Khandheria BK,Chandrasekaran K. Sildenafil citrate, a selective phosphodiesterase type 5 inhibitor: urologic and cardiovascular implications. World J Urol.2001 Feb;19(1):40-5.
 Moore RA,Edwards JE,McQuay HJ. Sildenafil (Viagra) for male erectile dysfunction: a meta-analysis of clinical trial reports. BMC Urol.2002 May 22;2:6.