Home Metabolism PDE inhibitor Sildenafil Citrate For research use only.

Sildenafil Citrate

Synonyms: UK-92480 Citrate

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.

Sildenafil Citrate Chemical Structure

Sildenafil Citrate Chemical Structure

CAS No. 171599-83-0

Purity & Quality Control

Sildenafil Citrate Related Products

Signaling Pathway

PDE Signaling Pathways

PDE Signaling Pathway

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
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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot HIF-1α / HIF-2α VEGF / PDK1 / CA9 p-AKT / AKT / p-mTOR / mTOR 23065129
In Vivo
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03686813 Completed
Edema Pulmonary|Immersion|Diving
Duke University|United States Department of Defense
 July 15 2019 Phase 2
NCT03417492 Terminated
Traumatic Brain Injury|Mild Traumatic Brain Injury|Post-Concussion Syndrome
University of Pennsylvania|Boston University
 March 1 2018 Phase 1
NCT03177824 Unknown status
Fetal Growth Restriction
Ain Shams University
 March 30 2017 Phase 3
NCT03262961 Unknown status
Pre-Eclampsia; Mild
Assiut University
 September 15 2016 Phase 2|Phase 3

Chemical Information & Solubility

Molecular Weight 666.7 Formula

C22H30N6O4S.C6H8O7
CAS No. 171599-83-0 SDF Download Sildenafil Citrate SDF
Smiles CCCC1=NN(C2=C1N=C(NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)C)OCC)C.C(C(=O)O)C(CC(=O)O)(C(=O)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 20 mg/mL ( (29.99 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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