Sildenafil Citrate

Catalog No.S1431
5 5 2 Product Citations

Sildenafil, 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

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Customer Reviews(1)

Quality Control & MSDS

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Product Information

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Product Description

Biological Activity

Description Sildenafil, 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] PDE6 [1]
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]
Features

Protocol(Only for Reference)

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

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
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

References

[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 http://clinicaltrials.gov, updated on 2014-11-22)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02060487 Recruiting Pulmonary Arterial Hypertension Pfizer September 2014 Phase 4
NCT01950923 Recruiting Kidney Tumor Comprehensive Cancer Center of Wake Forest University|Nat  ...more Comprehensive Cancer Center of Wake Forest University|National Cancer Institute (NCI) September 2013 --
NCT01996852 Recruiting Prostate Cancer|Erectile Dysfunction Following Radical Prostatectomy|Erectile Dysfunction Following Simple Prostatectomy|Erectile Dysfunction Case Comprehensive Cancer Center|The Cleveland Clinic|Uni  ...more Case Comprehensive Cancer Center|The Cleveland Clinic|University Hospital Case Medical Center July 2013 --
NCT01637675 Recruiting Pulmonary Hypertension|Pulmonary Arterial Hypertension|Cardiovascular Diseases|Lung Diseases|Tanshinone IIA Sulfonate The First Affiliated Hospital of Guangzhou Medical Univer  ...more The First Affiliated Hospital of Guangzhou Medical University|Jiangsu Carefree Pharmaceutical Co., LTD|The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School|Guangdong General Hospital|Sir run run shaw hospital Zhejiang University School of Medicine, Hangzhou, China|The First Affiliated Hospital of Zhengzhou University|Dongguan Peoples Hospital|Second Affiliated Hospital of Xian Jiaotong University|Beijing Chao Yang Hospital|Beijing Anzhen Hospital|Qingdao University May 2013 Phase 2|Phase 3
NCT01817751 Recruiting Glioblastoma Multiforme/Recurrent|Glioblastoma Multiforme|Meningioma Virginia Commonwealth University April 2013 Phase 2

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Chemical Information

Download Sildenafil Citrate SDF
Molecular Weight (MW) 666.7
Formula

C22H30N6O4S.C6H8O7

CAS No. 171599-83-0
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 23 mg/mL (34.49 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

Research Area

Customer Reviews (1)


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Rating
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.

Product Citations (2)

Tech Support & FAQs

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