|
Toll Free: (877) 796-6397 -- USA and Canada only -- |
Fax: +1-832-582-8590 Orders: +1-832-582-8158 |
Tech Support: +1-832-582-8158 Ext:3 Please provide your Order Number in the email. |
Technical Data
| Formula | C22H19N3O4 |
|||
| Molecular Weight | 389.4 | CAS No. | 171596-29-5 | |
| Solubility (25°C)* | In vitro | DMSO | 78 mg/mL (200.3 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
|
* <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. 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 | ||
|---|---|---|---|
| Targets |
|
||
| 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] | ||
| Features | Much more potent to PDE-5 than PDE-1 or PDE-6. |
Protocol (from reference)
| Animal Study: |
|
|---|
References
Customer Product Validation
-
Data from [Data independently produced by Cell Death Dis, 2014, 5, e1544]
-
Data from [Data independently produced by , , J Cell Physiol, 2015, 230(7): 1661-76]
Selleck's Tadalafil has been cited by 18 publications
| 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 |
| Impaired Redox and Protein Homeostasis as Risk Factors and Therapeutic Targets in Toxin-Induced Biliary Atresia [ Gastroenterology, 2020, 159(3):1068-1084.e2] | PubMed: 32505743 |
| Critical Impact of Drug-Drug Interactions via Intestinal CYP3A in the Risk Assessment of Weak Perpetrators Using Physiologically Based Pharmacokinetic Models. [ Drug Metab Dispos, 2020, 48(4):288-296] | PubMed: 31996361 |
| The role of PDE5a in oocyte maturation of zebrafish. [ Gen Comp Endocrinol, 2020, 286:113303] | PubMed: 31654676 |
| RhoBTB1 protects against hypertension and arterial stiffness by restraining phosphodiesterase 5 activity. [ J Clin Invest, 2019, 129(6):2318-2332] | PubMed: 30896450 |
| Phosphodiesterase 5 (PDE5) Is Highly Expressed in Cancer-Associated Fibroblasts and Enhances Breast Tumor Progression. [ Cancers (Basel), 2019, 11(11)] | PubMed: 31698786 |
| Activation of cGMP/PKG/p65 signaling associated with PDE5-Is downregulates CCL5 secretion by CD8 + T cells in benign prostatic hyperplasia [ Prostate, 2019, 79(8):909-919] | PubMed: 30958912 |
| Targeting the crosstalk between cytokine-induced killer cells and myeloid-derived suppressor cells in hepatocellular carcinoma [Yu SJ, et al. J Hepatol, 2018, 10.1016/j.jhep.2018.10.040] | PubMed: 30414862 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.