Sildenafil Citrate
For research use only.
Catalog No.S1431
15 publications

CAS No. 171599-83-0
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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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.
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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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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.
Purity & Quality Control
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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. | ||||||
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Targets |
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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] |
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Assay |
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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) |
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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 |
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Formula | C22H30N6O4S.C6H8O7 |
CAS No. | 171599-83-0 |
Storage |
powder in solvent |
Synonyms | N/A |
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) | ||||||||||
Dosage | mg/kg | Average weight of animals | g | Dosing volume per animal | ul | Number of animals | ||||
Step 2: Enter the in vivo formulation () | ||||||||||
% DMSO % % Tween 80 % ddH2O | ||||||||||
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: : mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL,)
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.
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.
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
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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 |
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.
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