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Formula | C22H19N3O4 |
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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) |
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* <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.) |
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 | ||
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Targets |
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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. |
Animal Study: |
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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]
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 |
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