Tadalafil

Catalog No.S1512 Synonyms: IC351

Tadalafil Chemical Structure

Molecular Weight(MW): 389.4

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

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In DMSO USD 140 In stock
USD 110 In stock
USD 170 In stock
USD 670 In stock
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2 Customer Reviews

  • (a): E. coli bacteria transformed to be resistant to ampicillin and kayamycin (AMPr KAYAr) were grown in AMPt KAYAt media and cells treated with OSU-03012 (2 μM); sildenafil (2 μM); tadalafil (2 μM), or in combination as indicated. Bacterial cell numbers were determined by assessing the protein concentration of the bacterial cell pellet 3 h, 6h and 12 h after drug exposure * P<0.05 less than corresponding vehicle value. The total protein content of each treatment condition was determined 3 h after addition of antibiotic. Portions of bacteria from each treatment condition were isolated and SDS PAGE and immuno-blotting performed to determine the expression of Dna J, Dna K, RecA and GrpE. (b): E. coli bacteria Gram stained and examined under a X100 oil immersion magnification.

    J Cell Physiol, 2015, 230(7): 1661-76. Tadalafil purchased from Selleck.

    β-Catenin levels in 293T cells treated with PDE5 inhibitor in the presence or absence of Wnt3a. (a) Tadalafil reduced β-catenin protein levels. Immunofluorescence and confocal images of 293T cells treated with dimethyl sulfoxide (DMSO) or tadalafil at 10 uM in the presence or absence of recombinant Wnt3a for 24 h.

    Cell Death Dis 2014 5, e1544. Tadalafil purchased from Selleck.

Purity & Quality Control

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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

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 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]

Protocol

Animal Research:

[3]

+ Expand
  • Animal Models: Sham-operated rats
  • Formulation: Saline
  • Dosages: 2 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL (200.3 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
30 mg/mL

* 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 Information

Molecular Weight 389.4
Formula

C22H19N3O4

CAS No. 171596-29-5
Storage powder
Synonyms IC351

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02891850 Recruiting Pulmonary Arterial Hypertension Bayer December 2016 Phase 4
NCT02682147 Not yet recruiting Emphysema University of Iowa|National Institutes of Health (NIH)|National Heart, Lung, and Blood Institute (NHLBI) November 2016 --
NCT02801032 Recruiting Stroke, Lacunar|Cerebral Small Vessel Diseases Christina Kruuse|Herlev Hospital July 2016 Phase 2
NCT02943356 Recruiting Erectile Dysfunction|Andropause The Catholic University of Korea|Hanmi Pharmaceutical Company Limited July 2016 Phase 4
NCT02819440 Recruiting Healthy|Obese Vanderbilt University July 2016 Phase 2
NCT02839122 Enrolling by invitation Benign Prostate Hyperplasia Yuyu Pharma, Inc. May 2016 Phase 1

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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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PDE Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID