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Sildenafil Citrate PDE inhibitor

Cat.No.S1431

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.
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Quality Control

Batch: Purity: 99.83%
99.83

Solubility

In vitro
Batch:

DMSO : 20 mg/mL (29.99 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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%
% Tween 80
% ddH2O
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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 666.7 Formula

C22H30N6O4S.C6H8O7

Storage (From the date of receipt)
CAS No. 171599-83-0 Download SDF Storage of Stock Solutions

Synonyms UK-92480 Citrate 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

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
PDE5
(Cell-free assay)
3.5 nM
PDE6
(Cell-free assay)
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.
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.
References

Applications

Methods Biomarkers Images PMID
Western blot HIF-1α / HIF-2α VEGF / PDK1 / CA9 p-AKT / AKT / p-mTOR / mTOR
S1431-WB1
23065129

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-05-11)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06800092 NOT_YET_RECRUITING
Cancer
The University of Texas Medical Branch, Galveston
2027-06-15 PHASE2; PHASE3
NCT06123156 RECRUITING
Rectal Cancer
University Hospital, Rouen
2025-09-25 PHASE3
NCT06510322 RECRUITING
Vascular Diseases
Montefiore Medical Center
2025-03-12 EARLY_PHASE1
NCT06649539 ACTIVE_NOT_RECRUITING
Peyronie Disease
Charitable Union for the Research and Education of Peyronie's Disease
2024-10-11 PHASE4
NCT07713914 RECRUITING
Pulmonary Arterial Hypertension (PAH)
University of Sao Paulo General Hospital
2026-07-22 PHASE4
NCT07039760 NOT_YET_RECRUITING
Brain Tumor
Washington University School of Medicine
2026-08-31 EARLY_PHASE1

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