1. Metabolic Enzyme/Protease
    Autophagy
  2. Phosphodiesterase (PDE)
    Autophagy

Sildenafil citrate (Synonyms: UK-92480 citrate)

Cat. No.: HY-15025A Purity: 99.53%
Data Sheet SDS Handling Instructions

Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.

For research use only. We do not sell to patients.
Sildenafil citrate Chemical Structure

Sildenafil citrate Chemical Structure

CAS No. : 171599-83-0

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Other Forms of Sildenafil citrate:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.

IC50 & Target

IC50: 5.22 nM (PDE 5)[1]

In Vitro

Pretreatment with 1 μM Sildenafil citrate potentiates the phosphorylation of ERK1/ERK2, an increase in the percentage of cells in S phase and cell proliferation, compared with serotonin stimulation alone (P<0.05). Pretreatment with 1 μM Sildenafil citrate followed by serotonin stimulation leads to dramatic increase in OD value to 0.33, significantly different compared with serotonin stimulation alone (P<0.05). 1 μM Sildenafil obviously enhances the upregulation of ERK1/ERK2 phosphorylation induced by serotonin[2].

In Vivo

In the dog model of erection, Sildenafil citrate significantly increases ICP and ICP/BP but shows no significant effect on BP compared with vehicle[1]. Sildenafil treatment significantly decreases the number of TL+-cells at 10 but not 0.5 mg/kg. At this time point, cells positive for the M1-like marker COX-2+ are found in the ischemic core in PBS-treated animals, whereas they are mostly observed in the penumbra in 10 mg/kg (but not 0.5 mg/kg) Sildenafil-treated animals. In contrast, 8 days after pMCAo the number of microglia/macrophages stained by Iba-1 are significantly reduced by Sildenafil treatment (0.5 and/or 10 mg/kg dose)[3]. Sildenafil citrate has been reported to decrease flap necrosis in preclinical animal models by increasing the secretion of growth factors (FGF and VEGF), and histologically is shown to be effective in rat cavernous nerve architecture[4].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01668446 farzaneh hojjat|Razieh dehghani firouzabadi|Robab davar|Shahid Sadoughi University of Medical Sciences and Health Services Endometrial Preparation|Frozen Embryo Transfer September 2009 Phase 4
NCT01889966 Kerckhoff Heart Center|Pfizer Pulmonary Hypertension Associated With Connective Tissue Disease April 2013 Phase 4
NCT00781508 MetroHealth Medical Center|National Center for Research Resources (NCRR) Heart Failure|Left Ventricular Dysfunction December 2006 Phase 4
NCT03229512 Northwestern University Hand Foot Skin Reaction April 11, 2017 Early Phase 1
NCT02136329 University of Leicester|British Heart Foundation Acute Kidney Injury June 2013 Phase 1
NCT01670136 University of North Carolina, Chapel Hill|Duke University|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|The EMMES Corporation Persistent Pulmonary Hypertension of the Newborn February 2013 Phase 1
NCT00527995 Ruhr University of Bochum Type 2 Diabetes Mellitus|Endothelial Dysfunction August 2001 Phase 3
NCT00800592 Pfizer Hypertension, Pulmonary October 2008 Phase 1
NCT01054001 Seoul National University Bundang Hospital|Pfizer Prostate Cancer June 2010
NCT00624273 Charite University, Berlin, Germany Active Digital Ulcers February 2004 Phase 2
NCT01954524 University of Maryland Cirrhosis May 2014 Phase 1
NCT00455715 Massachusetts General Hospital Schizophrenia February 2006 Phase 4
NCT00123162 Milton S. Hershey Medical Center|National Institutes of Health (NIH) Dysmenorrhea May 2007 Phase 1|Phase 2
NCT01060020 Washington University School of Medicine|Barnes-Jewish Hospital Aortic Stenosis January 2010 Phase 4
NCT01948518 The Cleveland Clinic Diffuse Parenchymal Lung Disease|Pulmonary Hypertension June 2009
NCT00692237 University of Roma La Sapienza Diabetes Mellitus, Type 2|Endothelial Dysfunction January 2008 Phase 4
NCT01046838 Jacob E Mueller|Rigshospitalet, Denmark Heart Failure, Diastolic December 2009 Phase 4
NCT00872170 New England Research Institutes|National Heart, Lung, and Blood Institute (NHLBI) Thalassemia|Hypertension, Pulmonary March 2009 Phase 2|Phase 3
NCT02304705 Maya Guglin|University of Kentucky Heart Failure With Reactive Pulmonary Hypertension January 2015 Phase 4
NCT02466802 Virginia Commonwealth University|Bayer Solid Tumor July 1, 2015 Phase 1
NCT01132482 National Jewish Health Cystic Fibrosis October 2015 Phase 2
NCT02277132 Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)|ZonMw: The Netherlands Organisation for Health Research and Development Fetal Growth Restriction January 2015 Phase 2|Phase 3
NCT00940901 Johns Hopkins University|National Institutes of Health (NIH) Sickle Cell Disease|Priapism June 2008 Phase 2
NCT00334490 St. Michael's Hospital, Toronto|University of Toronto Pulmonary Hypertension March 2005 Phase 2
NCT00808912 Marywood University Pulmonary Hypertension|Pulmonary Artery Pressure|Exercise Performance|Air Pollution December 2008
NCT01169519 Duke University Heart Disease April 2011 Phase 1
NCT00452582 Henry Ford Health System Ischemic Stroke April 2005 Phase 1
NCT01941732 Bispebjerg Hospital Parkinsons Disease|Erectile Dysfunction November 2003 Phase 4
NCT01347008 Federal University of São Paulo|Fundação de Amparo à Pesquisa do Estado de São Paulo Scleroderma, Systemic|Scleroderma, Diffuse|Scleroderma, Limited|Raynaud Phenomenon April 2011 Phase 3
NCT00964782 Penn State University|Children's Miracle Network Fontan Circulation August 2009 Phase 4
NCT02850718 iX Biopharma Ltd.|Linear Clinical Research Erectile Dysfunction March 2016 Phase 3
NCT00507819 Children's Hospital of Philadelphia|The Mark H. and Blanche M. Harrington Foundation Hypoplastic Left Heart Syndrome|Tricuspid Atresia December 2007 Phase 2
NCT02908490 University of Pittsburgh Arthritis, Rheumatoid|Atherosclerosis April 1, 2017 Phase 2
NCT03028298 University of Mississippi Medical Center Subarachnoid Hemorrhage|Cerebral Vasospasm December 2016 Phase 1
NCT00793338 University of New Mexico Heart Failure November 2008 Phase 4
NCT01757782 Sir Takhtasinhji General Hospital Meconium Aspiration Syndrome|Persistent Pulmonary Hypertension of Newborn December 2011 Phase 4
NCT01365585 Pfizer Pulmonary Arterial Hypertension July 2011
NCT01601470 Novartis Pharmaceuticals|Novartis Mild to Moderate Hypertension September 2012 Phase 2
NCT01616381 Helse Stavanger HF|Pfizer Heart Failure|Pulmonary Hypertension March 2013 Phase 3
NCT00866463 Pfizer Erectile Dysfunction October 2008 Phase 1
NCT02028429 Postgraduate Institute of Medical Education and Research Hepatic Encephalopathy. July 2012 Phase 1|Phase 2
NCT01091870 Hospital de Clinicas de Porto Alegre Subarachnoid Hemorrhage|Cerebral Vasospasm|Rupture of Intracranial Aneurysm March 2010 Phase 2
NCT02442492 University of British Columbia Intrauterine Growth Restriction (IUGR)|Fetal Growth Restriction (FGR) January 2017 Phase 2|Phase 3
NCT00517933 Duke University|National Heart, Lung, and Blood Institute (NHLBI)|Pfizer Pulmonary Fibrosis|Hypertension, Pulmonary August 2007 Phase 3
NCT00511498 Johns Hopkins University Prostate Cancer March 2006
NCT01290484 Stanford University Lymphangioma December 2010 Phase 1|Phase 2
NCT01108900 Pfizer Erectile Dysfunction July 2010 Phase 4
NCT01360671 Pfizer Persistent Pulmonary Hypertension of the Newborn March 2012 Phase 2
NCT01321489 Laboratório Teuto Brasileiro S/A Erectile Dysfunction September 2011 Phase 3
NCT03154476 Mayo Clinic Cirrhosis|Congenital Heart Disease July 2017 Early Phase 1
NCT02812433 McGill University Health Center Neonatal Encephalopathy July 2016 Phase 1
NCT01499498 Imperial College London Hepatitis C December 2012 Phase 1
NCT01247805 Pfizer Pulmonary Arterial Hypertention January 2011 Phase 1
NCT01055405 Hospital Clinic of Barcelona COPD|Pulmonary Hypertension August 2008 Phase 4
NCT02345980 Mansoura University Quality of Life March 2014 Phase 4
NCT01830790 Duke University Age-related Macular Degeneration March 2013 Phase 2
NCT01737203 Pfizer Healthy August 2012 Phase 1
NCT01107782 Tehran University of Medical Sciences Fetal Growth Retardation June 2008 Phase 2|Phase 3
NCT01168908 Hugo W. Moser Research Institute at Kennedy Krieger, Inc.|Johns Hopkins University Duchenne Muscular Dystrophy|Becker Muscular Dystrophy September 2010 Phase 2
NCT00710099 University Hospital, Grenoble Healthy July 2008
NCT02620995 National Institute of Cardiology, Laranjeiras, Brazil Arterial Hypertension|Erectile Dysfunction October 2014 Phase 4
NCT00730067 University of Aarhus|Aarhus University Hospital COPD|Pulmonary Hypertension June 2012 Phase 4
NCT01315262 Università Vita-Salute San Raffaele Erectile Dysfunction January 2011 Phase 3
NCT01194232 Children's Hospital Medical Center, Cincinnati Cystic Fibrosis With Mild to Moderate Lung Disease|CMRI of Lung Perfusion|Lung Perfusion|Lung Vascularization August 2012 Phase 1|Phase 2
NCT00133679 University of California, San Francisco|Children's Hospital Los Angeles|Ann & Robert H Lurie Children's Hospital of Chicago Hernia, Diaphragmatic|Hypertension, Pulmonary|Hypoplasia, Pulmonary February 2006 Phase 4
NCT00454207 Pfizer Pulmonary Hypertension April 2007 Phase 3
NCT01726049 University Medical Center Groningen|Pfizer Heart Failure, Diastolic|Pulmonary Hypertension October 2011 Phase 3
NCT00742014 The Hospital for Sick Children Hypertension August 2008 Phase 3
NCT01334554 Vanderbilt University Medical Center|National Heart, Lung, and Blood Institute (NHLBI)|Pfizer Metabolic Syndrome|Obesity April 2011 Phase 1|Phase 2
NCT02435303 Asan Medical Center Hypertension, Pulmonary|Diseases of Mitral Valve May 2016 Phase 2|Phase 3
NCT02106871 The University of Texas Medical Branch, Galveston Pancreatic Cancer|Cholangiocarcinoma April 2014 Phase 1
NCT03177824 Ain Shams University Fetal Growth Restriction March 30, 2017 Phase 3
NCT02590536 Ain Shams University Fetal Growth Retardation October 2015 Phase 3
NCT02832570 University Hospital, Angers Peripheral Arterial Occlusive Disease August 2016 Phase 3
NCT00586794 Competence Network for Congenital Heart Defects|German Federal Ministry of Education and Research Pulmonary Arterial Hypertension (PAH) December 2007 Phase 3
NCT00814736 Pfizer Prostatic Hyperplasia|Urinary Bladder, Overactive|Erectile Dysfunction August 2008 Phase 1
NCT02114775 The University of Texas Medical Branch, Galveston Traumatic Brain Injury March 2015 Phase 1
NCT00104637 Kawut, Steven, MD|Pfizer Pulmonary Disease, Chronic Obstructive|Emphysema February 2005 Phase 2
NCT01375699 Virginia Commonwealth University Breast Cancer|Gastrointestinal Cancer|Genitourinary Cancer|Sarcoma|Gynecologic Cancer August 11, 2011 Phase 1
NCT02710981 Assiut University Anovulation June 2015
NCT02162979 Loma Linda University Parkinson's Disease February 2002 Phase 2
NCT01762475 Uniformed Services University of the Health Sciences|Center for Neuroscience and Regenerative Medicine (CNRM)|National Institute of Neurological Disorders and Stroke (NINDS)|National Institutes of Health (NIH) Traumatic Brain Injury|Post-concussive Syndrome January 2013 Phase 2
NCT02628847 University of Utah Stroke March 2012 Phase 1
NCT01352507 Eli Lilly and Company Erectile Dysfunction June 2011 Phase 4
NCT00359736 VA Office of Research and Development Alveolitis, Fibrosing|Fibrosis, Pulmonary|Hypertension, Pulmonary July 2006 Phase 2
NCT00165295 Dana-Farber Cancer Institute|Beth Israel Deaconess Medical Center Waldenstrom's Macroglobulinemia September 2005 Phase 2
NCT01720524 Pfizer Pulmonary Hypertension, Familial Persistent, of the Newborn August 5, 2013 Phase 3
NCT00431418 Mercy Hospital for Women, Australia Lung Diseases January 2007 Phase 3
NCT00795938 Pfizer Erectile Dysfunction October 2008 Phase 1
NCT01295736 University Hospital, Lille Systemic Scleroderma November 2010 Phase 3
NCT01441934 Italian Association of Hospital Pneumologists Pulmonary Hypertension|COPD October 2010 Phase 3
NCT00746967 Pfizer Sexual Dysfunctions, Psychological|Sexual Arousal Disorder January 2003 Phase 2
NCT01382368 Rabin Medical Center Chronic Obstructive Pulmonary Disease|Idiopathic Pulmonary Fibrosis September 2011 Phase 4
NCT02782559 The University of Texas Health Science Center, Houston Preterm Preeclampsia July 2016 Phase 2|Phase 3
NCT02845388 Omar Ahmed El Sayed Saad|Ain Shams Maternity Hospital Infertility September 2015 Phase 2
NCT03142568 University of North Carolina, Chapel Hill|Duke University|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|The EMMES Corporation Bronchopulmonary Dysplasia August 2017 Phase 2
NCT01642407 Pfizer Pulmonary Arterial Hypertension|Hypertension, Pulmonary August 24, 2012 Phase 3
NCT00547287 Eli Lilly and Company|ICOS Corporation Impotence November 2002 Phase 3
NCT02930811 University Hospital, Angers Peripheral Arterial Occlusive Disease June 2017 Phase 3
NCT02519153 Mansoura University Ureteral Stone|Urolithiasis July 2014 Phase 4
NCT02335242 Stanford University|Ann & Robert H Lurie Children's Hospital of Chicago Lymphatic Malformations|Lymphatic Diseases May 23, 2015 Phase 2
NCT01254383 Pfizer Erectile Dysfunction December 2010 Phase 1
NCT00491803 Hospital Clinic of Barcelona Chronic Obstructive Pulmonary Disease|Pulmonary Hypertension June 2007 Phase 4
NCT00625079 University of California, Los Angeles|Pfizer Pulmonary Arterial Hypertension|Idiopathic Pulmonary Fibrosis|Interstitial Lung Disease|Pulmonary Hypertension February 2007 Phase 4
NCT00659529 National Jewish Health|Cystic Fibrosis Foundation Therapeutics Cystic Fibrosis August 2008 Phase 1|Phase 2
NCT01185925 University of Milan Heart Failure April 2008 Phase 2
NCT02372487 Al Hayat National Hospital|Menoufia University Pregnancy Complication March 2015
NCT03169582 Eduardo Vargas-Baquero|Hospital Nacional de Parapléjicos de Toledo Erectile Dysfunction April 1, 2016 Phase 4
NCT02983461 The University of Texas Medical Branch, Galveston Urinary Incontinence March 10, 2017 Phase 1
NCT01853540 National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) Nontuberculous Mycobacterial Infection January 2013 Phase 1|Phase 2
NCT01950923 Wake Forest University Health Sciences|National Cancer Institute (NCI) Kidney Tumor September 2013 Phase 2
NCT02524184 Xiang Guang-da|Wuhan General Hospital of Guangzhou Military Command Obesity August 2015 Phase 4
NCT01409031 University of Colorado, Denver|National Heart, Lung, and Blood Institute (NHLBI)|State University of New York at Buffalo|Vanderbilt University|Ann & Robert H Lurie Children's Hospital of Chicago|University of Utah|University of Alabama at Birmingham Persistent Pulmonary Hypertension|Respiratory Failure July 2011 Phase 2
NCT01936350 Hospital Ana Nery Heart Failure September 2013 Phase 2|Phase 3
NCT01254396 Pfizer Erectile Dysfunction December 2010 Phase 1
NCT00862043 Hospital General Universitario Gregorio Marañon|Instituto de Salud Carlos III|Fundación de Investigación en Red en Enfermedades Cardiovasculares Pulmonary Hypertension|Valvular Heart Disease April 2009 Phase 4
NCT02387450 University Hospital, Angers Peripheral Arterial Disease September 2015 Phase 2|Phase 3
NCT01897740 Pfizer Pulmonary Arterial Hypertension (PAH)
NCT03192709 Royan Institute|Tehran University of Medical Sciences Infertility, Female February 2015 Phase 1|Phase 2
NCT02060487 Pfizer Pulmonary Arterial Hypertension September 22, 2014 Phase 4
NCT01392638 University of Campinas, Brazil|Fundação de Amparo à Pesquisa do Estado de São Paulo Hypertension July 2010
NCT02050360 University Hospital, Grenoble Raynaud's Phenomenon November 2013 Phase 2|Phase 3
NCT02378649 Dr. Robert Klempfner Heart Rehabilitation Institute|Sheba Medical Center Pulmonary Hypertension|Mitral Valve Surgery March 2015 Phase 4
NCT00902512 Pfizer|Investigacion Farmacologica y Biofarmaceutica, S.A. de C.V. Healthy Males April 2009 Phase 4
NCT00763867 Duke University|National Heart, Lung, and Blood Institute (NHLBI)|Pfizer Heart Failure September 2008 Phase 3
NCT01219023 Duke University Hand Foot Syndrome|Palmar Plantar Erythrodysesthesia June 2010 Phase 1
NCT01091012 Hospital Universitari Vall d'Hebron Research Institute Pulmonary Hypertension September 2011 Phase 3
NCT02595541 Assiut University Pulmonary Hypertension June 2015 Phase 1|Phase 2
NCT00309816 Massachusetts General Hospital Congestive Heart Failure December 2001 Phase 3
NCT00492531 National Heart, Lung, and Blood Institute (NHLBI) Sickle Cell Disease|Pulmonary Hypertension June 2007 Phase 2
NCT00627965 Altitude Physiology Expeditions|University of Edinburgh High Altitude Pulmonary Edema|Acute Mountain Sickness March 2003 Phase 4
NCT02244528 Seoul National University Hospital|Seoul National University Bundang Hospital Neonates and Preterm Infants October 2014 Phase 2
NCT01481350 University of Turin, Italy Pulmonary Hypertension February 2012 Phase 2
NCT00780728 University Health Network, Toronto Hypertension, Pulmonary Phase 3
NCT00142506 Memorial Sloan Kettering Cancer Center|Icahn School of Medicine at Mount Sinai|Beth Israel Medical Center|St. Luke's-Roosevelt Hospital Center Prostate Cancer|Erectile Dysfunction February 2005 Phase 3
NCT00866983 Pfizer Pulmonary Arterial Hypertension October 2009
NCT01817751 Virginia Commonwealth University|National Cancer Institute (NCI) Glioblastoma|Glioma|Recurrent Adult Brain Neoplasm April 11, 2013 Phase 2
NCT03027674 Pontificia Universidad Catolica de Chile Raynaud Phenomenon Due to Trauma|Raynaud Disease|System; Sclerosis|Lupus Erythematosus, Systemic|Dermatomyositis|Ultrasound Therapy; Complications August 2016 Early Phase 1
NCT00666198 Pfizer Pulmonary Hypertension May 2008
NCT02890238 Cairo University Infertility August 2016 Phase 4
NCT02951429 Hoffmann-La Roche Idiopathic Pulmonary Fibrosis January 13, 2017 Phase 2
NCT00904748 Pfizer Erectile Dysfunction January 2010 Phase 1
NCT02663830 Ain Shams University Anovulatory January 2016 Phase 2
NCT02390960 Strategic Science & Technologies, LLC Erectile Dysfunction March 2015 Phase 2
NCT00454714 Udo Sechtem|Robert Bosch Gesellschaft für Medizinische Forschung mbH Coronary Vasospasm March 1, 2007 Phase 3
NCT02939495 Neutec Ar-Ge San ve Tic A.Ş Premature Ejaculation|Erectile Dysfunction October 2016 Phase 4
NCT01373749 Third Military Medical University|National Natural Science Foundation of China Persistent Pulmonary Hypertension of Newborn March 2011
NCT00654017 Pfizer Erectile Disfunction|Hemodialysis October 2002 Phase 4
NCT01419392 Ain Shams University Recurrent Miscarriage September 2011 Phase 4
NCT01800292 University of Arizona Hypertension, Pulmonary Artery|Ventricular Dysfunction, Left February 2013 Phase 4
NCT00878943 Pfizer Pulmonary Arterial Hypertension April 2009
NCT00547092 Eli Lilly and Company|ICOS Corporation Impotence October 2003 Phase 4
NCT00645034 Pfizer Benign Prostatic Hyperplasia November 2002 Phase 2
NCT00975494 University of Milan Heart Failure April 2005 Phase 3
NCT01986673 Strategic Science & Technologies, LLC Healthy October 2013 Phase 1
NCT01558466 Hamad Medical Corporation Persistent Fetal Circulation Syndrome November 2011 Phase 3
NCT00796666 Pfizer Pulmonary Arterial Hypertension|Pulmonary Hypertension May 2009 Phase 3
NCT00547352 Eli Lilly and Company|ICOS Corporation Impotence June 2004 Phase 4
NCT00483626 University of Chile Pulmonary Arterial Hypertension August 2003 Phase 4
NCT00159809 Pfizer Impotence|Depression March 2004 Phase 4
NCT00350441 NHS Greater Glasgow Yorkhill Division Cardiopulmonary Bypass June 2006 Phase 4
NCT00479908 University of Edinburgh|Pfizer Angina Pectoris January 2004 Phase 4
NCT01661595 The University of Texas Medical Branch, Galveston Fatigue November 2012
NCT03185364 Chinese Academy of Medical Sciences, Fuwai Hospital COPD|Pulmonary Hypertension June 15, 2017
NCT00871065 University of Nebraska Cerebral Vasospasm|Subarachnoid Hemorrhage July 2009 Phase 2
NCT00159874 Pfizer Pulmonary Arterial Hypertension January 2004 Phase 3
NCT00468650 Pfizer Erectile Dysfunction June 2007 Phase 4
NCT02795351 Herlev Hospital Migraine With Aura June 2015 Early Phase 1
NCT00796510 Pfizer Pulmonary Arterial Hypertension|Pulmonary Hypertension July 2010 Phase 3
NCT00937144 The Baruch Padeh Medical Center, Poriya Sickle Cell Anemia September 2009 Phase 4
NCT00145483 Pfizer Meniere's Disease June 2002 Phase 2
NCT00599235 University of Edinburgh Hypertension March 2007
NCT00145938 University of Chicago Pulmonary Hypertension September 2003 Phase 2
NCT00317421 University of Edinburgh|Pfizer Hypertension March 2004 Phase 2
NCT03044561 Ain Shams University IVF Failure January 31, 2017 Phase 4
NCT02362399 Al Hayat National Hospital|Menoufia University Pregnancy Complication March 2015
NCT00309790 Massachusetts General Hospital Congestive Heart Failure May 2003 Phase 3
NCT01350154 Rigshospitalet, Denmark|Glostrup University Hospital, Copenhagen Becker Muscular Dystrophy November 2011 Phase 2
NCT00375297 University of New Mexico|Pfizer Sexual Dysfunction|Depression January 2001 Phase 4
NCT01517854 University Health Network, Toronto Portopulmonary Hypertension October 2012 Phase 2
NCT00343200 Pfizer Impotence July 2006 Phase 4
NCT00302211 Actelion Pulmonary Hypertension February 2006 Phase 3
NCT02364882 Strategic Science & Technologies, LLC Female Sexual Health January 2015 Phase 1
NCT01656798 Pfizer Healthy August 2012 Phase 1
NCT00640458 Pfizer Female Sexual Arousal Disorder April 2004 Phase 2
NCT01179334 Bayer Pulmonary Hypertension August 2010 Phase 2
NCT00251784 University of Cambridge Blindness February 2002 Phase 4
NCT00159861 Pfizer Pulmonary Hypertension July 2003 Phase 3
NCT02766725 Assiut University Infertility January 2015 Phase 2|Phase 3
NCT01359670 Cedars-Sinai Medical Center|Parent Project Muscular Dystrophy Duchenne Muscular Dystrophy May 2011
NCT00645268 Pfizer Erectile Dysfunction|Diabetes Mellitus, Type 2 December 2002 Phase 4
NCT00644631 Pfizer Erectile Dysfunction June 2003 Phase 4
NCT00175981 Heidelberg University Healthy February 2003 Phase 1
NCT00141310 Pfizer Pre-Eclampsia September 2004 Phase 2
NCT00644956 Pfizer Erectile Dysfunction June 2003 Phase 4
NCT00352482 National Heart, Lung, and Blood Institute (NHLBI) Pulmonary Fibrosis|Hypertension, Pulmonary November 2004 Phase 2
NCT00946114 Pfizer Pulmonary Hypertension June 2006
NCT02626182 National Jewish Health Cystic Fibrosis December 2015 Phase 1|Phase 2
NCT00598585 Charles Drew University of Medicine and Science|Pfizer Chronic Fatigue Syndrome July 2002 Phase 4
NCT01812434 University of Minnesota - Clinical and Translational Science Institute Cardiac Allograft Vasculopathy October 2010
NCT00303004 Rigshospitalet, Denmark Eisenmenger Syndrome March 2006 Phase 3
NCT00159887 Pfizer Pulmonary Hypertension December 2002 Phase 3
NCT01244620 Pfizer Pulmonary Arterial Hypertension November 2010 Phase 1
NCT02802345 Boehringer Ingelheim Idiopathic Pulmonary Fibrosis June 30, 2016 Phase 3
NCT03199612 Montefiore Medical Center Thrombosis|Hemolysis August 1, 2017 Early Phase 1
NCT00147628 Pfizer Impotence November 2005 Phase 4
NCT00159913 Pfizer Pulmonary Arterial Hypertension, Children August 2003 Phase 3
NCT00815646 Duke University|Divers Alert Network Immersion Pulmonary Edema (IPE)|Swimming Induced Pulmonary Edema (SIPE) January 2008 Early Phase 1
NCT01572363 Universitaire Ziekenhuizen Leuven Congenital Heart Disease April 2012
NCT00654082 Pfizer Spinal Cord Injury|Erectile Dysfunction|Spinal Cord Trauma|Injuries, Spinal Cord|Impotence September 2002 Phase 4
NCT00430716 Pfizer Pulmonary Arterial Hypertension April 2008 Phase 4
NCT00818701 Mayo Clinic Congestive Heart Failure|Renal Dysfunction February 2009 Phase 1
NCT00463957 University of Cambridge Erectile Dysfunction August 2006
NCT02337881 Al Hayat National Hospital|Menoufia University Labor Preterm Requiring Hospitalization January 2015 Phase 1
NCT00768573 Pfizer None Volunteer January 2008 Phase 1
NCT00323297 Pfizer Pulmonary Arterial Hypertension September 2006 Phase 4
NCT00644605 Pfizer Hypertension, Pulmonary October 2002 Phase 3
NCT01582438 Pfizer Pulmonary Arterial Hypertension November 2012
NCT00655590 Bayer Erectile Dysfunction January 2005 Phase 4
NCT00057759 Radiation Therapy Oncology Group|National Cancer Institute (NCI) Prostate Cancer|Psychosocial Effects of Cancer and Its Treatment|Radiation Toxicity|Sexual Dysfunction|Sexuality and Reproductive Issues January 2003
NCT00245258 Pfizer Impotence November 2005 Phase 4
NCT01616485 VIVUS, Inc. Erectile Dysfunction March 2004 Phase 1
NCT00407446 University of Milan Heart Failure January 2004 Phase 3
NCT00752115 Hamamatsu University Non-small Cell Lung Cancer February 2007 Phase 2|Phase 3
NCT00544076 City of Hope Medical Center Prostate Cancer|Male Erectile Disorder|Stage I Prostate Cancer|Stage II Prostate Cancer January 2006
NCT00143260 Pfizer Impotence August 2005 Phase 4
NCT00249730 Pfizer Impotence October 2005 Phase 4
NCT02990078 University of Pennsylvania TBI December 2016
NCT03053739 Postgraduate Institute of Medical Education and Research Associated Pulmonary Arterial Hypertension December 2016 Phase 4
NCT00194909 Weill Medical College of Cornell University|Pfizer Diabetic Neuropathy August 2004 Phase 4
NCT02678221 Assiut University Intrauterine Growth Restriction February 2016 Phase 2
NCT00151463 Pfizer Impotence January 2005 Phase 4
NCT00194597 University of Washington|Berger, Richard E., M.D. Prostatitis July 2004 Phase 4
NCT02057458 National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) Cystic Fibrosis April 2014 Phase 2
NCT00150358 Pfizer Impotence|Hypertension March 2005 Phase 4
NCT01637675 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|The First Affiliated Hospital of Zhengzhou University|Dongguan People's Hospital|Second Affiliated Hospital of Xi'an Jiaotong University|Beijing Chao Yang Hospital|Beijing Anzhen Hospital|Qingdao University Pulmonary Hypertension|Pulmonary Arterial Hypertension|Cardiovascular Diseases|Lung Diseases|Tanshinone IIA Sulfonate May 2013 Phase 2|Phase 3
NCT03012386 Vanderbilt University Medical Center|Washington University School of Medicine Insulin Resistance|Endothelial Dysfunction January 2017 Phase 1|Phase 2
NCT00137072 Pfizer Impotence April 2005 Phase 4
NCT00155714 National Taiwan University Hospital Primary and Secondary Pulmonary Hypertension November 2002
NCT01913847 Hanmi Pharmaceutical Company Limited Pulmonary Hypertension|Systolic Dysfunction September 2013 Phase 3
NCT00772135 Oslo University Hospital|Norwegian Foundation for Health and Rehabilitation|Pfizer Congenital Heart Disease September 2008
NCT00313898 Rambam Health Care Campus|Pfizer Erectile Dysfunction September 2005 Phase 4
NCT00301262 Pfizer Impotence November 2005 Phase 4
NCT01391104 Laval University Pulmonary Arterial Hypertension April 2009
NCT01059994 The University of Texas Medical Branch, Galveston Fatigue|Aging January 2010
NCT02975037 Seoul National University Hospital Healthy December 2016 Phase 4
NCT02798159 Vietstar Biomedical Research Erectile Dysfunction May 2016 Phase 2|Phase 3
NCT00159900 Pfizer Erectile Dysfunction May 2005 Phase 4
NCT02129725 Vanderbilt University Medical Center Metabolic Syndrome April 2014 Phase 4
NCT00906269 Hartford Hospital Impotence|Prostatic Neoplasms July 2009 Phase 4
NCT00955929 Memorial Sloan Kettering Cancer Center|Pfizer Penile Cancer|Erectile Dysfunction|Radical Prostatectomy August 2009
NCT01122264 Eli Lilly and Company Erectile Dysfunction May 2010 Phase 4
NCT02682147 University of Iowa|National Institutes of Health (NIH)|National Heart, Lung, and Blood Institute (NHLBI) Emphysema July 10, 2017 Phase 4
NCT00512707 Boston University|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) Erectile Dysfunction|Testosterone Deficiency|Diabetes November 2006 Phase 4
NCT00461565 Bayer|GlaxoSmithKline Safety February 2005 Phase 4
NCT00433329 Actelion Pulmonary Arterial Hypertension March 2007 Phase 4
NCT00273416 Pfizer Impotence January 2006 Phase 2
NCT02546609 NuSirt Biopharma NAFLD November 2015 Phase 2
NCT00056433 National Institutes of Health Clinical Center (CC) Sickle Cell Anemia March 10, 2003 Phase 1
NCT00648596 Pfizer Erectile Dysfunction May 2003 Phase 4
NCT00420901 IRCCS San Raffaele Diabetes January 1999 Phase 3
NCT01153204 Federal University of São Paulo|University of Sao Paulo Erectile Dysfunction Phase 4
NCT00498680 Rambam Health Care Campus Impotence March 2007 Phase 4
NCT00245596 Pfizer Impotence October 2005 Phase 4
NCT00981747 University of Iowa|Pulmonary Fibrosis Foundation Idiopathic Pulmonary Fibrosis|Pulmonary Fibrosis September 2009 Phase 2|Phase 3
NCT03143465 Danish Headache Center Migraine With Aura August 2016
NCT01548950 University of Sao Paulo General Hospital|Instituto do Coracao|Fundação de Amparo à Pesquisa do Estado de São Paulo Congenital Heart Disease|Pulmonary Arterial Hypertension September 2011
NCT01364701 Rambam Health Care Campus Erectile Dysfunction June 2011 Phase 4
NCT02946944 Meshalkin Research Institute of Pathology of Circulation Pulmonary Embolism|Intermediate-high Risk|Combination of Oral Anticoagulation Therapy and Sildenafil October 2016 Phase 1
NCT01156636 University of Milan Pulmonary Hypertension|Diastolic Heart Failure January 2006 Phase 2|Phase 3
NCT01996852 Case Comprehensive Cancer Center|The Cleveland Clinic|University Hospitals Cleveland Medical Center Prostate Cancer|Erectile Dysfunction Following Radical Prostatectomy|Erectile Dysfunction Following Simple Prostatectomy|Erectile Dysfunction July 2013
NCT00862888 Pfizer Erectile Dysfunction July 2007 Phase 2
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NCT01449253 All India Institute of Medical Sciences, New Delhi Pulmonary Hypertension Secondary to Lung Disease and/or Hypoxia August 2011 Phase 4
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.4999 mL 7.4996 mL 14.9992 mL
5 mM 0.3000 mL 1.4999 mL 2.9998 mL
10 mM 0.1500 mL 0.7500 mL 1.4999 mL
Cell Assay
[2]

Sildenafil is prepared in DMSO and stored, and then diluted with appropriate medium before use[2].

Cells at approximately 90% confluence are harvested with 0.1% trypsin/0.01% ethylene diamine tetraacetic acid (EDTA) solution and seeded into a 96-well plate at a density of 2×104 cells/well and grown in RPMI-1640 containing 10% FBS for three days, followed by serum starvation for three days. Cells are then incubated for different time with various concentration of serotonin or 1 μM Sildenafil followed by serotonin with or without U0126, as indicated. Control cells are treated in the same way except sterile PBS replaced the drug. After treatment, medium is changed to fresh medium, and cells are incubated with 5 g/L of MTT for four hours. MTT is then dissolved with 150 μL of 10% DMSO for 20 minutes. The optical densities (OD) in the 96-well plates are determined using a microplate reader at 570 nm[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3][4]

Sildenafil citrate is prepared in PBS.

Mice[3]
Ischemia is induced in C57Bl/6 mice on postnatal (P) day 9 by permanent middle cerebral artery occlusion (pMCAo), and followed by either PBS or Sildenafil intraperitoneal (i.p.) injections. In the first set of experiments, animals are randomly divided into five groups and treated with either PBS or a single dose of Sildenafil citrate (0.5, 2.5, 10, and 15 mg/kg), given intraperitoneally (i.p.) 5 min after pMCAo. In the second set of experiments, animals are randomly divided into three groups and treated with either PBS or a single dose of Sildenafil citrate (0.5 and 10 mg/kg, i.p.) 5 min after pMCAo.
Rat[4]
Thirty male Sprague-Dawley rats weighing between 210 and 240 g are used. Rats from all groups are anesthetized with xylazine + ketamine and then a crush injury is created by using a one-minute long vascular clamp to the right sciatic nerve. One day before the procedure, rats from Group 1 are started on a 28-day treatment consisting of a daily dose of 20 mg/kg body weight Sildenafil given orally via nasogastric tube, while the rats from Group 2 are started on an every-other-day dose of 10 mg/kg body weight Sildenafil citrate. Rats from Group 3 did not receive any drugs. Subjects in all 3 groups are fed ad libitum with normal rat chow and tap water. Forty-two days after the nerve damage is created, the rats underwent a static sciatic index (SSI) test, sedation and motor coordination tests, and accelerated rotarod tests. Rats are sacrificed under anesthesia and their sciatic nerves are removed surgically. Histopathologic analyses of the nerves and bone densitometry evaluation of the extremities are then performed. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

666.7

Formula

C₂₈H₃₈N₆O₁₁S

CAS No.

171599-83-0

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 29 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Sildenafil citrate
Cat. No.:
HY-15025A
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