Sildenafil Citrate

Catalog 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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Sildenafil Citrate Chemical Structure

Sildenafil Citrate Chemical Structure
Molecular Weight: 666.7

Validation & Quality Control

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Related Compound Libraries

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Product Description

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)
IC50 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]
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]

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Nehra A, et al. World J Urol, 2001, 19(1), 40-45.

[2] Shukla N, et al. Eur J Pharmacol, 2005, 517(3), 224-231.

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Clinical Trial Information( data from, updated on 2016-07-23)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02798159 Recruiting Erectile Dysfunction Vietstar Biomedical Research May 2016 Phase 2|Phase 3
NCT02678221 Not yet recruiting Intrauterine Growth Restriction Assiut University February 2016 Phase 2
NCT02590536 Not yet recruiting Fetal Growth Retardation Ain Shams University October 2015 Phase 3
NCT02466802 Recruiting Solid Tumor Virginia Commonwealth University|Bayer July 2015 Phase 1
NCT02372487 Recruiting Pregnancy Complication Al Hayat National Hospital|Menoufia University March 2015 --

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Chemical Information

Download Sildenafil Citrate SDF
Molecular Weight (MW) 666.7


CAS No. 171599-83-0
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 20 mg/mL warming (29.99 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name 1-[[3-(6,7-Dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-ethoxyphenyl]sulfonyl]-4-methylpiperazine, 2-hydroxy-1,2,3-propanetricarboxylate

Customer Product Validation(2)

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Source Mol Pharmacol 2014 5(3), 408-19. Sildenafil Citrate purchased from Selleck
Method Immunoblotting
Cell Lines T24 cells
Concentrations 2 uM
Incubation Time 6/12 h
Results Sildenafil combinated with doxorubicin significantly increased the phosphorylation of γhistone 2AX (γH2AX) 6 and 12 hours after exposure.

Click to enlarge
Source J Cell Physiol 2014 10.1002/jcp.24843. Sildenafil Citrate purchased from Selleck
Method Immunohistochemistry
Cell Lines BT549, HOSS1 cells
Concentrations 2 uM
Incubation Time 6 h
Results In further agreement with a role for CD95 in the killing process, sildenafil combination with celecoxib exposure caused a rapid plasma membrane localization and clustering of CD95, indicative of receptor activation.

Tech Support

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