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Vardenafil-d5

Names

[ CAS No. ]:
1189685-70-8

[ Name ]:
Vardenafil-d5

[Synonym ]:
Vardenafil-d5
Nuviva-d5
Imidazo[5,1-f][1,2,4]triazin-4(1H)-one, 2-[2-ethoxy-5-[[4-(ethyl-d)-1-piperazinyl]sulfonyl]phenyl]-5-methyl-7-propyl-
Levitra-d5
2-(2-Ethoxy-5-{[4-(H)ethyl-1-piperazinyl]sulfonyl}phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(1H)-one

Biological Activity

[Description]:

Vardenafil-d5 is deuterium labeled Vardenafil. Vardenafil is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction[1][2].

[Related Catalog]:

Research Areas >> Endocrinology
Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)

[In Vitro]

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

[References]

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

[2]. Ashour AE, et al. Vardenafil dihydrochloride. Profiles Drug Subst Excip Relat Methodol. 2014;39:515-544.

[3]. 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):282-290.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
692.3±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C23H27D5N6O4S

[ Molecular Weight ]:
493.63

[ Flash Point ]:
372.5±34.3 °C

[ Exact Mass ]:
493.251953

[ PSA ]:
121.28000

[ LogP ]:
2.65

[ Vapour Pressure ]:
0.0±2.2 mmHg at 25°C

[ Index of Refraction ]:
1.656

Related Compounds