Home Metabolism PDE inhibitor Sildenafil For research use only.

Sildenafil

Synonyms: Revatio, UK-92480, Viagra

Sildenafil (Revatio, UK-92480, Viagra) is a Phosphodiesterase 5 Inhibitor with IC50 of 5.22 nM.

Sildenafil Chemical Structure

Sildenafil Chemical Structure

CAS: 139755-83-2

Selleck's Sildenafil has been cited by 20 Publications

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Purity & Quality Control

Batch: Purity: 99.97%
99.97

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human erythrocytes Function assay 60 mins Inhibition of ABCC5 in human erythrocytes assessed as inhibition of ATP-mediated [3H]cGMP uptake in inside-out vesicles after 60 mins by liquid scintillation counting, Ki=1.2 μM 22380603
HEK293 Function assay TP_TRANSPORTER: inhibition of 9-(2-phosphonomethoxyethyl)adenine(PMEA) efflux (PMEA: 1 uM) in MRP4-expressing HEK293 cells, IC50=20μM 12695538
mammalian cells Function assay Inhibition of human Potassium channel HERG expressed in mammalian cells, IC50=3.31131μM 12873512
RFL-6 Function assay Inhibition of phosphodiesterase 5 in rat fetal lung fibroblast (RFL-6) cells, Ki=0.0018μM 15771456
CHO Function assay Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique, IC50=3.31131μM 18448342
COS7 Function assay Inhibition of human recombinant PDE5A1 expressed in COS7 cells, IC50=0.075μM 18778098
HEK293T Function assay 2 hrs Displacement of [3H]ZM241385 from human AA2AR expressed in HEK293T cells after 2 hrs by liquid scintillation counter, Ki=0.19953μM 22563707
HEK293T Function assay 45 mins Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis, IC50=4.5μM 23122865
Sf9 Function assay Inhibition of human PDE5A1 expressed in baculovirus in sf9 cells by PDE Glo phosphodiesterase assay, IC50=0.0056μM 25801159
BL21-CodonPlus(DE3) Function assay 30 mins Inhibition of human His-tagged PDE5A catalytic domain expressed in Escherichia coli BL21-CodonPlus(DE3) cells using [3H]cAMP or [3H]cGMP as substrate incubated for 30 mins by scintillation counting method, IC50=0.0022μM 26908025
Sf9 Function assay 15 mins Inhibition of recombinant human PDE5A1 catalytic domain (535 to 860 residues) expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate incubated for 15 mins by liquid scintillation counting method, IC50=0.0022μM 26908025
BL21-CodonPlus Function assay Inhibition of recombinant human His6-tagged PDE5A (535 to 786 residues)/PDE6C expressed in Escherichia coli BL21-CodonPlus cells using [3H]cGMP as substrate, Ki=0.025μM 26908025
BL21-CodonPlus(DE3) Function assay 30 mins Inhibition of human His-tagged PDE4B catalytic domain expressed in Escherichia coli BL21-CodonPlus(DE3) cells using [3H]cAMP or [3H]cGMP as substrate incubated for 30 mins by scintillation counting method, IC50=20μM 26908025
Sf9 Function assay 30 mins Inhibition of full length recombinant human N-terminal GST-tagged PDE5A1 expressed in baculovirus infected Sf9 cells using cGMP as substrate after 30 mins by HTRF assay, IC50=0.004μM 27606546
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
Sf9 Function assay 1 hr Inhibition of N-terminal GST-tagged full length recombinant human PDE5A1 catalytic domain expressed in Baculovirus infected Sf9 insect cells using FAM-cGMP as substrate after 1 hr by fluorescence polarization assay, IC50=0.00365μM 29505934
Sf9 Function assay 30 mins Inhibition of N-terminal GST-tagged human PDE5A1 expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay, IC50=0.00431μM 31021628
Sf9 Function assay 30 mins Inhibition of N-terminal GST-tagged human PDE6C expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay, IC50=0.03642μM 31021628
Sf9 Function assay 30 mins Inhibition of N-terminal GST-tagged human PDE1 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay, IC50=0.819μM 31021628
Sf9 Function assay 30 mins Inhibition of N-terminal GST-tagged human PDE11A4 expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay, IC50=4.93μM 31021628
Click to View More Cell Line Experimental Data

Biological Activity

Description Sildenafil (Revatio, UK-92480, Viagra) is a Phosphodiesterase 5 Inhibitor with IC50 of 5.22 nM.
Targets
PDE5 [1]
5.22 nM
In vitro
In vitro Sildenafil improves insulin signalling and NO production in endothelial cells, probably by reducing oxidative stress induced by hyperglycemia and by increasing intracellular Ca2+ levels[2].
Cell Research Cell lines HUVEC and HAEC
Concentrations 1 μM
Incubation Time 5 or 72 h
Method

HUVEC and HAEC from passages 3 to 6 are cultured for 72 hours in presence of 5.5 mmol/L glucose, 30 mmol/L glucose (high glucose; HG), 10 mmol/L Gluc-N with or without 1 µM of sildenafil (5 or 72 h) and/or 10−7 M insulin.
In Vivo
In vivo Acute administration of the PDE-5 inhibitor sildenafil in a single clinically relevant dose does not modulate the in vivo function of the hypertrophic failing right heart of the rat measured by echocardiography and invasive hemodynamics[1].
Animal Research Animal Models Wistar rats
Dosages 1 mg/kg
Administration i.v.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05466695 Not yet recruiting Erectile Dysfunction and Neutrophil Lymphocyte Ratio Assiut University August 1 2022 Early Phase 1
NCT05275725 Recruiting Birth Asphyxia Pia Wintermark|Kawempe National Referral Hospital|Saint Francis Memorial Hospital|Walimu|McGill University Health Centre/Research Institute of the McGill University Health Centre July 1 2022 Phase 1
NCT04565925 Recruiting Spinal Cord Injuries|Urinary Incontinence The University of Texas Medical Branch Galveston July 7 2021 Phase 2
NCT04122105 Unknown status Renal Transplant Failure University of British Columbia April 1 2021 Not Applicable

Chemical lnformation & Solubility

Molecular Weight 474.58 Formula

C22H30N6O4S
CAS No. 139755-83-2 SDF Download Sildenafil SDF
Smiles CCCC1=NN(C2=C1N=C(NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)C)OCC)C
Storage (From the date of receipt)

In vitro
Batch:

Water : 14 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble


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In vivo
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