Cell lines

human hepatocytes

Preparation method

The solubility of this compound in DMSO is >16.6mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1 μM

Applications

Tadalafil (1 μM) increased CYP3A protein expression in human hepatocytes.

Animal models

Rat model with bilateral cavernous neurotomy (BCN)-induced penile damage and hypo-oxygenation, Mice with cavernous nerve resection

Dosage form

2 mg/kg, daily for 3 months

Application

Tadalafil (2 mg/kg) almost completely restored penile oxygenation and abolished neurotomy induced increase and substantially rescued muscle/fiber ratio in penile sectionsin sham-operated rats. Tadalafil decreased the number of apoptotic cells and increased the phosphorylation of the 2 survival associated kinases Akt and extracellular signal-regulated kinase 1/2 in mice.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

Tadalafil, also known as IC351 or Cialis, is a potent, reversible and competitive small-molecule inhibitor of phosphodiesterase 5 (PDE5), a predomiant PDE in the pulmonary vasculature that hydrolyzes cyclic guanosine monophosphate (cGMP) and is involved in the pathobiology of pulmonary arterial hypertension (PAH). 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.

Reference

[1].Fusae Sawamura, Masami Kato, Kazushisa Fujita, Takahiro Nakazawa and Anthony Bearsworth. Tadalafil, a long-acting inhibitor of PDE5, improves pulmonary hemodynamics and survival rate of monocrotaline-induced pulmonary artery hypertension in rats. J Pharmacol Sci 111, 235-243 (2009)
[2].H Porst. IC351 (tadalafil, Cialis): update on clinical experience. Internation Journal of Impotence Research (2002) 14, Suppl 1, S57-S64
[3].S. Thomas Forgue, Beverley E. Patterson, Alun W. Bedding, Christopher D. Payne, Diane L. Phillips, Rebecca E. Wrishko and Malcolm I. Mitchell. Tadalafil pharmacokinetics in healthy subjects. Br J Clin Pharmacol (2005); 61(3): 280-288