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 No. 139755-83-2

Purity & Quality Control

Sildenafil Related Products

Signaling Pathway

PDE Signaling Pathways

PDE Signaling Pathway

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 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

Chemical Information & 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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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.

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