product name Tadalafil
Description: Tadalafil, also known as IC351 or Cialis, is a potent, reversible and competitive small-molecule inhibitor of PDE-5 with IC50 of 1.8 nM in a cell-free assay. The inhibitory effect of tadalafil is PDE5 specific with the selectivity of 10000 times greater than that of PDE1, PDE4, PDE7, PDE8, PDE9 and PDE10 and of 780 times greater than that of PDE6. Although it is used for the treatment of erectile dysfunction through oral administration, tadalafil also improves the vasoconstrictive-predominate condition of PAH through elevating cGMP levels in pulmonary vessels resulted from PDE5 inhibition.
References: Mol Pharmacol. 2004;66(1):144-52; Clin Pharmacol Ther. 2005;77(1):63-75; J Sex Med. 2006;3(3):419-31.
389.4
Formula
C22H19N3O4
CAS No.
171596-29-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 78 mg/mL (200.3 mM)
Water: <1 mg/mL
Ethanol: 50 mg/mL (145.6 mM)
Solubility (In vivo)
30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
Synonyms
IC351
other peoduct :
| In Vitro |
In vitro activity: Tadalafil binds to PDE5 with KD of 2.4 nM. cGMP stimulates the binding of [3H]Tadalafil. Tadalafil (1 mM) results increased CYP3A protein expression in human hepatocytes Kinase Assay: Cell Assay: |
|---|---|
| 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. 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. 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 |
| Animal model | Sham-operated rats |
| Formulation & Dosage | Dissovled in saline; 2 mg/kg; oral gavage |
| References | Mol Pharmacol. 2004 Jul;66(1):144-52; Clin Pharmacol Ther. 2005 Jan;77(1):63-75; J Sex Med. 2006 May;3(3):419-31. |
3-O-(2-Aminoethyl)-25-hydroxyvitamin D5
