Sildenafil Citrate

Name: Sildenafil Citrate
Brand: Selleck Chemicals
SKU: S1431
Rating: 5 (15 reviews)

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.

Selleck's Sildenafil Citrate has been cited by 15 publications

J Clin Invest, 2021, 131(1)136779

PubMed: 33393490 ( click the link to review the publication )

Sci Rep, 2020, 10(1):18084

PubMed: 33093580 ( click the link to review the publication )

Cancers (Basel), 2019, 11(11)

PubMed: 31698786 ( click the link to review the publication )

Hypertension, 2018, 72(1):167-176

PubMed: 29735634 ( click the link to review the publication )

Cancer Lett, 2016, 370(2):279-85

PubMed: 26551887 ( click the link to review the publication )

J Cell Physiol, 2016, 231(10):2286-302

PubMed: 27187154 ( click the link to review the publication )

Pharm Dev Technol, 2016, 21(8):961-971

PubMed: 26428267 ( click the link to review the publication )

Oncotarget, 2016, 7(11):12975-96

PubMed: 26887051 ( click the link to review the publication )

J Cell Physiol, 2015, 10.1002/jcp.24961

PubMed: 25704960 ( click the link to review the publication )

J Cell Physiol, 2015, 230(5):1115-27

PubMed: ( click the link to review the publication )

J Cell Physiol, 2015, 10.1002/jcp.24977

PubMed: 25736380 ( click the link to review the publication )

Mol Pharmacol, 2014, 85(3):408-19

PubMed: 24353313 ( click the link to review the publication )

J Cell Physiol, 2014, 10.1002/jcp.24919

PubMed: 25546329 ( click the link to review the publication )

Cancer Biol Ther, 2014, 15(6):758-67

PubMed: 24651037 ( click the link to review the publication )

Daru, 2013, 21(1):68

PubMed: 24355133 ( click the link to review the publication )

3 Customer Reviews

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.
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

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 ; PubMed: 23065129 Am J Respir Cell Mol Biol Sildenafil up-regulated HIF-1α and HIF-2α in a dose-dependent manner. Human small airway epithelial (HSAEp-C) cells were incubated with the indicated concentrations of sildenafil for 16 hours, and the expression of HIF-1/2α was evaluated by Western blotting. VEGF / PDK1 / CA9 ; PubMed: 23065129 Am J Respir Cell Mol Biol Semiquantitative RT-PCR of HIF-target gene transcripts in HSAEp-C cells. Cells were incubated with 100 μM sildenafil for the indicated times, and total RNAs were extracted. The mRNA concentrations of VEGF, pyruvate dehydrogenase kinase (PDK), carbonic anhydrase 9 (CA9), and HIF-1α were analyzed by RT-PCR with deoxycytidine 5′-[α-32P] triphosphate and autoradiographed. The result is representative of three experiments. p-AKT / AKT / p-mTOR / mTOR ; PubMed: 23065129 Am J Respir Cell Mol Biol Sildenafil activated the AKT/mTOR signaling pathway. HSAEp-C cells were incubated with 100 μM sildenafil for the indicated times, and then harvested to determine protein concentrations by Western blotting.	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

References

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 Download Sildenafil Citrate SDF

Molecular Weight	666.7
Formula	C₂₂H₃₀N₆O₄S.C₆H₈O₇
CAS No.	171599-83-0
Storage	3 years-20°C powder 2 years-80°C 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)

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mg/kg

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Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% 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， 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.

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.

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).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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 (data from https://clinicaltrials.gov, updated on 2020-01-06)

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

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

Tel: +1-832-582-8158 Ext:3

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Sildenafil Citrate