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Sildenafil mesylate

Catalog No.
PDE5 inhibitor
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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 [1].

In vivo: In anesthetized dogs, sildenafil could enhance the erectile function following pelvic nerve stimulation as measured by increased intracavernosal pressure [1].

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 [2].

[1] 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.
[2] 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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
Cas No.1308285-21-3
Solubility≥57.1mg/mL in DMSO
Chemical Name5-(2-ethoxy-5-((4-methylpiperazin-1-yl)sulfonyl)phenyl)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one methanesulfonate
SDFDownload SDF
Canonical SMILESCCCC(C(N=C(N1)C2=C(OCC)C=CC(S(N3CCN(CC3)C)(=O)=O)=C2)=C4C1=O)=NN4C.CS(O)(=O)=O
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Chemical structure

Sildenafil mesylate