Sildenafil Citrate

Catalog No.S1431

Sildenafil Citrate Chemical Structure

Molecular Weight(MW): 666.7

Sildenafil Citrate, a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5), is a well-tolerated and highly effective treatment for erectile dysfunction.

Size Price Stock Quantity  
In DMSO USD 90 In stock
USD 70 In stock
USD 110 In stock
USD 670 In stock
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3 Customer Reviews

  • ADOR lung cancer cells (a July 2015 PDX model) were transfected with an empty vector plasmid or plasmids to express GRP78 and HSP27 together. Twenty-four hours after transfection cells were treated with vehicle control or with OSU-03012 (2.0mM) sildenafil (2mM) for 6 h after which cells were fixed in place and permeabilized using 0.5% Triton X100. Immuno-fluorescence was performed to detect the expression levels of Calnexin; glucosidase I; and glucosidase IIa at 10 magnification using a Hermes WiScan system.

    J Cell Physiol, 2016, 231(10):2286-302. . Sildenafil Citrate purchased from Selleck.

    T24 cells were treated with vehicle, SIL (2 uM), DOX (200 nM) as indicated. Cells were isolated 6 and 12 hours after exposure, and the phosphorylation of γH2AX was determined, with the fold increase in phosphorylation shown.

    Mol Pharmacol 2014 5(3), 408-19. Sildenafil Citrate purchased from Selleck.

  • BT549 and HOSS1 cells in 96 well plates were treated with celecoxib (CEL 5.0 uM) and/or sildenafil (SIL, 2.0 uM). Six h after treatment cells were fixed to the plate and immunohistochemistry performed to determine the plasma membrane levels of CD95. The upper images obtained using the Hermes Wiscan imaging system is representative of the data. The intensity of CD95 immunostaining was determined using the Wisoft data analysis package (n = 3 +/- SEM). * p < 0.05 value greater than celecoxib treatment alone.

    J Cell Physiol 2014 10.1002/jcp.24843. Sildenafil Citrate purchased from Selleck.

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Biological Activity

Description Sildenafil Citrate, a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5), is a well-tolerated and highly effective treatment for erectile dysfunction.
Targets
PDE5 [1]
(Cell-free assay)
PDE6 [1]
(Cell-free assay)
3.5 nM 33 nM
In vitro

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. [1]

In vivo Sildenafil citrate enhances erectile function following pelvic nerve stimulation in anesthetized dogs as measured by increased intracavernosal pressure. [1] Sildenafil citrate significantly reverses impaired carbachol-stimulated relaxation and inhibits superoxide formation by cavernosal tissue from hypercholesterolaemic rabbits. [2] 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. [3]

Protocol

Solubility (25°C)

In vitro DMSO 20 mg/mL warmed (29.99 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 666.7
Formula

C22H30N6O4S.C6H8O7

CAS No. 171599-83-0
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03044561 Recruiting IVF Failure Ain Shams University January 31, 2017 Phase 4
NCT03012386 Not yet recruiting Insulin Resistance|Endothelial Dysfunction Vanderbilt University Medical Center|Washington University School of Medicine January 2017 Phase 1|Phase 2
NCT03028298 Recruiting Subarachnoid Hemorrhage|Cerebral Vasospasm University of Mississippi Medical Center December 2016 Phase 1
NCT02990078 Not yet recruiting TBI University of Pennsylvania December 2016 --
NCT02890238 Not yet recruiting Infertility Cairo University August 2016 Phase 4
NCT02798159 Recruiting Erectile Dysfunction Vietstar Biomedical Research May 2016 Phase 2|Phase 3

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PDE Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID