Vardenafil hydrochloride

  • CasNo:224785-91-5
  • Molecular Formula:C23H33ClN6O4S
  • Purity:
  • Molecular Weight:
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Product Details

224785-91-5 Name

Name

Vardenafil hydrochloride

Synonym

1-[[3-(1,4-dihydro-5-methyl-4-oxo-7-propylimidazo[5,1-f][1,2,4]triazin-2-yl)-4-ethoxyphenyl]sulfonyl]-4-ethyl-piperazine dihydrochloride;2-[2-Ethoxy-5-(4-ethylpiperazin-1-yl)sulfonylphenyl]-5-methyl-7-propyl-1H-imidazo[5,1-f][1,2,4]triazin-4-one hydrochloride;vardenafil hydrochloride;VARDENAFIL HCL;Vardenafil Hydrochloride Trihydrate 224785-90-4 /;Levitra,Valdenafil.HCl;1-[[3-(1,4-Dihydro-5-methyl-4-oxo-7-propylimidazo[5,1-f][1,2,4]triazin-2-yl)-4-ethoxyphenyl]sulfonyl]-4-ethyl-piperazine;Nuviva

 

224785-91-5 Biological Activity

Description

Vardenafil Hcl is a PDE5 inhibitor used for treating erectile dysfunction.Target: PDE5Vardenafil specifically inhibited the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM (6.6 nM). In contrast, the IC50 of vardenafil for PDE1 was 180 nM; for PDE6, 11 nM; for PDE2, PDE3 and PDE4, more than 1000 nM. Relative to PDE5, the ratios of the IC50 for PDE1 were 257 (60), for PDE6 16 (7.4). Vardenafil significantly enhanced the SNP-induced relaxation of human trabecular smooth muscle at 3 nM (10 nM). Vardenafil also significantly potentiated both ACh-induced and transmural electrical stimulation-induced relaxation of trabecular smooth muscle [1]. 

Related Catalog

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

Research Areas >> Cardiovascular Disease

References

[1]. Saenz de Tejada, I., et al., The phosphodiesterase inhibitory selectivity and the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Int J Impot Res, 2001. 13(5): p. 282-90.

[2]. Goldstein, I., et al., Vardenafil, a new phosphodiesterase type 5 inhibitor, in the treatment of erectile dysfunction in men with diabetes: a multicenter double-blind placebo-controlled fixed-dose study. Diabetes Care, 2003. 26(3): p. 777-83.

 

224785-91-5 Chemical & Physical Properties

Melting point 

214-216ºC

Boiling point

692.2ºC at 760 mmHg

Molecular Formula

C23H33ClN6O4S

Molecular Weight

525.064

Flash Point

372.5ºC

PSA

121.28000

LogP

3.82900

Exact Mass

524.197266

Vapour Pressure

5.17E-19mmHg at 25°C

 

224785-91-5 Description

Vardenafil was the second agent to be marketed and had the advantage that its onset time was not reduced by taking the medication on a full stomach . It is 30 times more potent as an inhibitor of PDE5 (mean IC50, 3.9 nM) than sildenafil and 10 times more potent than tadalafil, with a greater selectivity (>1,000 times) for human PDE5 than for human PDE2, PDE3, and PDE4 and moderate selectivity (>80 times) for PDE1. The PDE inhibitory selectivity and both the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Vardenafil specifically inhibited the hydrolysis of cGMP by PDE5, with an IC50 of 0.7 nM (sildenafil 6.6 nM). The IC50 of vardenafil for PDE1 was 180 nM, for PDE6 11 nM, and for PDE2, PDE3 and PDE4 more than 1,000 nM.

 

224785-91-5 Uses

vardenafil hydrochloride is a selective phsphodiesterase type 5 (pde5) inhibitor that is used as a urological agent in the treatment of erectile dysfunction.