Tadalafil

Catalog No.S1512 Batch:S151204

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Technical Data

Formula

C22H19N3O4
Molecular Weight 389.4 CAS No. 171596-29-5
Solubility (25°C)* In vitro DMSO 88 mg/mL (225.98 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 3.900mg/ml (10.02mM) Taking the 1 mL working solution as an example, add 50 μL of clarified DMSO stock solution of 78 mg/ml to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Tadalafil is a PDE-5 inhibitor with IC50 of 1.8 nM in a cell-free assay. This compound 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
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]this compound. This chemical (1 mM) results increased CYP3A protein expression in human hepatocytes.
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. This compound (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. It selectively increases cGMP but not cAMP in brain of rats. It 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.
Features Much more potent to PDE-5 than PDE-1 or PDE-6.

Protocol (from reference)

Animal Study:

[3]
  • Animal Models

    Sham-operated rats

  • Dosages

    2 mg/kg

  • Administration

    Orally

References

  • https://pubmed.ncbi.nlm.nih.gov/15213306/
  • https://pubmed.ncbi.nlm.nih.gov/15637532/
  • https://pubmed.ncbi.nlm.nih.gov/16681467/
  • https://pubmed.ncbi.nlm.nih.gov/16959227/
  • https://pubmed.ncbi.nlm.nih.gov/18082193/

Customer Product Validation

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.

Data from [ Cell Death Dis , 2014 , 5, e1544 ]

(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.

Data from [ , , J Cell Physiol, 2015, 230(7): 1661-76 ]

Selleck's Tadalafil Has Been Cited by 25 Publications

Phosphodiesterase 5 (PDE5) Is Highly Expressed in Cancer-Associated Fibroblasts and Enhances Breast Tumor Progression [ Cancers, November 06, 2019, 1740] PubMed: 31698786
Phosphodiesterase Inhibitors Sildenafil and Vardenafil Reduce Zebrafish Rod Photoreceptor Outer Segment Shedding [ Investigative Ophthalmology & Visual Science, November 01, 2017, 5604-5615] PubMed: 29094165
Phosphodiesterase Inhibitors Sildenafil and Vardenafil Reduce Zebrafish Rod Photoreceptor Outer Segment Shedding [ Investigative Ophthalmology & Visual Science, November 01 2017, 5604-5615] PubMed: 29094165
Targeting the crosstalk between cytokine-induced killer cells and myeloid-derived suppressor cells in hepatocellular carcinoma [ Journal of Hepatology, March 2019, 449-457] PubMed: 30414862
Evaluation of Sildenafil and Tadalafil for Reversing Constriction of Fetal Arteries in a Human Placenta Perfusion Model [ Hypertension, July 2018, 167-176]
Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805] PubMed: 39581704
Pharmacologically increasing cGMP improves proteostasis and reduces neuropathy in mouse models of CMT1 [ Cell Mol Life Sci, 2024, 81(1):434] PubMed: 39400753
RGS2-mediated translational control mediates cancer cell dormancy and tumor relapse [ J Clin Invest, 2021, 131(1)136779] PubMed: 33393490
Tadalafil enhances the therapeutic efficacy of BET inhibitors in hepatocellular carcinoma through activating Hippo pathway [ Biochim Biophys Acta Mol Basis Dis, 2021, 1867(12):166267] PubMed: 34508829
Tadalafil impacts the mechanical properties of Plasmodium falciparum gametocyte-infected erythrocytes [ Mol Biochem Parasitol, 2021, 244:111392] PubMed: 34171456

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.