Home Metabolism PDE inhibitor Tadalafil For research use only.

Tadalafil

Synonyms: IC351

Tadalafil is a PDE-5 inhibitor with IC50 of 1.8 nM in a cell-free assay. Tadalafil is at least 9000 times more selective for PDE5 than most of the other families of PDEs, with the exception of PDE11. It can partial inhibits PDE11

Tadalafil Chemical Structure

Tadalafil Chemical Structure

CAS: 171596-29-5

Selleck's Tadalafil has been cited by 18 Publications

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Purity & Quality Control

Batch: Purity: 100%
100

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Biological Activity

Description Tadalafil is a PDE-5 inhibitor with IC50 of 1.8 nM in a cell-free assay. Tadalafil is at least 9000 times more selective for PDE5 than most of the other families of PDEs, with the exception of PDE11. It can partial inhibits PDE11
Features Much more potent to PDE-5 than PDE-1 or PDE-6.
Targets
PDE5 [1]
(Cell-free assay)
1.8 nM
In vitro
In vitro Tadalafil binds to PDE5 with KD of 2.4 nM. cGMP stimulates the binding of [3H]Tadalafil. [1] Tadalafil (1 mM) results increased CYP3A protein expression in human hepatocytes. [2]
In Vivo
In vivo Tadalafil (2 mg/kg) almost completely restores penile oxygenation and abolishes neurotomy induced increase and substantially rescues muscle/fiber ratio in penile sectionsin sham-operated rats. [3] Tadalafil (2 mg/kg or 10 mg/kg) significantly improves neurological functional recovery and increases cerebral vascular density and the percentage of BrdU-positive endothelial cells around the ischemic boundary. Tadalafil selectively increases cGMP but not cAMP in brain of rats. [4] Tadalafil decreases the number of apoptotic cells and increases the phosphorylation of the 2 survival associated kinases Akt and extracellular signal-regulated kinase 1/2 in mice. [5]
Animal Research Animal Models Sham-operated rats
Dosages 2 mg/kg
Administration Orally
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05884957 Recruiting Erectile Dysfunction|Diabetes Mellitus Egymedicalpedia June 1 2023 Not Applicable
NCT05709574 Recruiting Gastric Adenocarcinoma|Gastroesophageal Junction Adenocarcinoma University of Arizona March 3 2023 Phase 2
NCT05466695 Not yet recruiting Erectile Dysfunction and Neutrophil Lymphocyte Ratio Assiut University August 1 2022 Early Phase 1
NCT05173896 Recruiting Cerebral Small Vessel Diseases|Stroke Ischemic Christina Kruuse|Danish Research Centre for Magnetic Resonance|Bispebjerg Hospital|Rigshospitalet Denmark|Hillerod Hospital Denmark|University of Copenhagen|The Novo Nordic Foundation|Herlev Hospital May 31 2022 Phase 2
NCT05195775 Recruiting Duchenne Muscular Dystrophy University of Florida December 14 2021 Phase 2|Phase 3

Chemical lnformation & Solubility

Molecular Weight 389.4 Formula

C22H19N3O4
CAS No. 171596-29-5 SDF Download Tadalafil SDF
Smiles CN1CC(=O)N2C(C1=O)CC3=C(C2C4=CC5=C(C=C4)OCO5)NC6=CC=CC=C36
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 78 mg/mL ( (200.3 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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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