Home Metabolism PDE inhibitor Sildenafil Citrate

Sildenafil Citrate

Catalog No.S1431

For research use only.

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

CAS No. 171599-83-0

Selleck's Sildenafil Citrate has been cited by 18 publications

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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]
Assay
Methods Test Index PMID
Western blot HIF-1α / HIF-2α ; VEGF / PDK1 / CA9 ; p-AKT / AKT / p-mTOR / mTOR 23065129
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 (from reference)

Solubility (25°C)

In vitro

 DMSO 20 mg/mL warmed
(29.99 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.

 30 mg/mL

* 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 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03417492 Recruiting Drug: Sildenafil Citrate Traumatic Brain Injury|Mild Traumatic Brain Injury|Post-Concussion Syndrome University of Pennsylvania|Boston University March 1 2018 Phase 1
NCT03177824 Unknown status Drug: Sildenafil Citrate 25Mg Tab|Drug: Placebo Oral Tablet Fetal Growth Restriction Ain Shams University March 30 2017 Phase 3
NCT03262961 Unknown status Drug: Sildenafil 20 MG|Drug: Placebo Oral Tablet Pre-Eclampsia; Mild Assiut University September 15 2016 Phase 2|Phase 3
NCT00165295 Completed Drug: Sildenafil citrate (Viagra) Waldenstrom''s Macroglobulinemia Dana-Farber Cancer Institute|Beth Israel Deaconess Medical Center September 2005 Phase 2

(data from https://clinicaltrials.gov, updated on 2021-09-06)

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