Cialis

Modify Date: 2024-01-02 04:35:05

Cialis structure	Common Name	Cialis
	CAS Number	171596-29-5	Molecular Weight	389.404
	Density	1.5±0.1 g/cm3	Boiling Point	679.1±55.0 °C at 760 mmHg
	Molecular Formula	C₂₂H₁₉N₃O₄	Melting Point	298-300ºC
	MSDS	N/A	Flash Point	364.5±31.5 °C
	Symbol	GHS02, GHS07	Signal Word	Danger

Use of Cialis

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

Name	tadalafil
Synonym	More Synonyms

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 >> Phosphodiesterase (PDE) Research Areas >> Cardiovascular Disease
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.

Description

Related Catalog

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)

Research Areas >> Cardiovascular Disease

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.

Density	1.5±0.1 g/cm3
Boiling Point	679.1±55.0 °C at 760 mmHg
Melting Point	298-300ºC
Molecular Formula	C₂₂H₁₉N₃O₄
Molecular Weight	389.404
Flash Point	364.5±31.5 °C
Exact Mass	389.137543
PSA	74.87000
LogP	1.43
Vapour Pressure	0.0±2.1 mmHg at 25°C
Index of Refraction	1.758
Storage condition	Hygroscopic, -20?C Freezer, Under Inert Atmosphere

Symbol	GHS02, GHS07
Signal Word	Danger
Hazard Statements	H225-H302 + H312 + H332-H319
Precautionary Statements	P210-P261-P302 + P352 + P312-P304 + P340 + P312-P337 + P313-P403 + P235
Hazard Codes	F,Xn
Risk Phrases	11-20/21/22-36
Safety Phrases	16-36/37
RIDADR	UN 1648 3 / PGII

Precursor 7
CAS#:1224724-00-8 (1R,3R)-methyl-... CAS#:74-89-5 methylamine CAS#:171489-59-1 Chloropretadalafil CAS#:14907-27-8 H-D-Trp-OMe.HCl
CAS#:52605-49-9 H-Sar-Oet·HCl CAS#:120-57-0 piperonal CAS#:171596-41-1 (1R,2S,3R)-(+)-...
DownStream 2
CAS#:171596-27-3 12-epi-Tadalafi... CAS#:1220393-12-3 (3R)-3-[[2-(1,3...