171596-29-5

171596-29-5 Biological Activity

Description

Tadalafil is a PDE5 inhibitor with an IC50 value of 1.8 nM.IC50 Value: 1.8±0.4nM [1]Target: PDE 5Tadalafil is marketed in pill form for treating erectile dysfunction(ED) under the name Cialis, and under the name Adcirca for the treatment of pulmonary arterial hypertension. Tadalafil can elevate the level of cGMP in the corpus cavernosum and effectively improve ED of various causes and degrees.in vitro: Biochemical potencies (affinities) of these compounds for PDE5 determined by IC(50), K(D) (isotherm), K(D) (dissociation rate), and K(D) ((1/2) EC(50)), respectively, were the following: sildenafil (3.7 +/- 1.4, 4.8 +/- 0.80, 3.7 +/- 0.29, and 11.7 +/- 0.70 nM), tadalafil (1.8 +/- 0.40, 2.4 +/- 0.60, 1.9 +/- 0.37, and 2.7 +/- 0.25 nM); and vardenafil (0.091 +/- 0.031, 0.38 +/- 0.07, 0.27 +/- 0.01, and 0.42 +/- 0.10 nM). Thus, absolute potency values were similar for each inhibitor, and relative potencies were vardenafil >> tadalafil > sildenafil [1]. 0.5 ml tadalafil solutions with different concentrations were added (0.2, 0.1, 0.05 and 0.025 μg ml-1, respectively) into semen samples. In both groups, samples treated with 0.2 μg ml-1 tadalafil had significant increase in sperm motility after 2 h incubation [2].in vivo: The Tadalafil-treated group showed enhanced erectile function (intracavernosal pressure/mean arterial pressure) at 0.3, 0.5, 1, 3, and 5 Hz compared with diabetic group values at the respective frequencies (P <.05) that approached control values [3]. oral administration of tadalafil (20 mg) or sildenafil (100 mg) was given. In both groups, computer-assisted semen analysis parameters showed no significant difference. After the administration of tadalafil (2 h) and sildenafil (1 h), there was no significant difference observed in premature acrosome reaction incidence rate [2].Clinical trial: Study the Safety and Effectiveness of Tadalafil in Men With Problems Getting or Maintaining an Erection When Taken Prior to Desiring an Erection. Phase 3

Related Catalog

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodies

References

[1]. Blount MA, et al. Binding of tritiated sildenafil, tadalafil, or vardenafil to the phosphodiesterase-5 catalytic site displays potency,specificity, heterogeneity, and cGMP stimulation. Mol Pharmacol. 2004 Jul;66(1):144-52.

[2]. Yang Y, et al. Effect of acute tadalafil on sperm motility and acrosome reaction: in vitro and in vivo studies. Andrologia. 2013 Apr 14. [Epub ahead of print]

[3]. Mostafa ME, et al. Effect of Chronic Low-dose Tadalafil on Penile Cavernous Tissues in Diabetic Rats. Urology. 2013 Jun;81(6):1253-60.

171596-29-5 Chemical & Physical Properties

Melting point 

298-300ºC

Boiling point

679.1±55.0 °C at 760 mmHg

Density

1.5±0.1 g/cm3

Molecular Formula

C22H19N3O4

Molecular Weight

389.404

Flash Point

PSA

74.87000

LogP

1.43

Exact Mass

389.137543

Vapour Pressure

0.0±2.1 mmHg at 25°C

Index of Refraction

1.758

Storage condition

Hygroscopic, -20?C Freezer, Under Inert Atmosphere