224785-90-4

224785-90-4 structure

Name: Vardenafil
Chemical Name: vardenafil
CAS Number: 224785-90-4
Molecular Formula: C₂₃H₃₂N₆O₄S
Molecular Weight: 488.60
Catalog: Biochemical Inhibitor Metabolism PDE inhibitor
Create Date: 2018-02-07 08:00:00
Modify Date: 2024-01-02 12:04:29
Vardenafil 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]. Both vardenafil doses(10 mg or 20 mg) significantly enhanced the rates of successful penetration (P < 0.0001) and successful intercourse (P < 0.0001) compared with placebo. Vardenafil treatment was effective in increasing intercourse success rates at all levels of baseline ED severity, at each level of plasma HbA1c, and for type 1 and 2 diabetes [2].

Name	vardenafil
Synonyms	Vardenafil (INN) Vivanza 2-{2-Ethoxy-5-[(4-ethylpiperazin-1-yl)sulfonyl]phenyl}-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(1H)-one 4-[2-ethoxy-5-(4-ethyl-piperazine-1-sulfonyl)-phenyl]-9-methyl-7-propyl-3,5,6,8-tetrazabicyclo[4.3.0]nona-3,7,9-trien-2-one Vardenafil hydrochloride trihydrate [14C]-Vardenafil 2-{2-Ethoxy-5-[(4-ethyl-1-piperazinyl)sulfonyl]phenyl}-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(1H)-one 2-[2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonylphenyl]-5-methyl-7-propyl-1H-imidazo[5,1-f][1,2,4]triazin-4-one Vardenafil HCl Trihydrate 4-[2-eyhoxy-5-(4-ethylpiperazin-1-yl)sulfonyl-phenyl]-9-methyl-7-propyl-3,5,6,8-tetrazabicyclo[4,3,0] none 3,7,9 trien-2-one Imidazo[5,1-f][1,2,4]triazin-4(3H)-one, 2-[2-ethoxy-5-[(4-ethyl-1-piperazinyl)sulfonyl]phenyl]-5-methyl-7-propyl- vardenafil Levitra (TN)

Description	Vardenafil 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]. Both vardenafil doses(10 mg or 20 mg) significantly enhanced the rates of successful penetration (P < 0.0001) and successful intercourse (P < 0.0001) compared with placebo. Vardenafil treatment was effective in increasing intercourse success rates at all levels of baseline ED severity, at each level of plasma HbA1c, and for type 1 and 2 diabetes [2].
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE) Research Areas >> Endocrinology
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.

Density	1.4±0.1 g/cm3
Boiling Point	692.2ºC at 760mmHg
Melting Point	214-216ºC
Molecular Formula	C₂₃H₃₂N₆O₄S
Molecular Weight	488.60
Flash Point	372.5ºC
PSA	121.28000
LogP	2.65
Vapour Pressure	5.17E-19mmHg at 25°C
Index of Refraction	1.656
Storage condition	?20°C

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	UN1230 - class 3 - PG 2 - Methanol, solution

5308-25-8

224789-21-3

224785-90-4

Literature: US2007/197535 A1, ; Page/Page column 6 ;

5308-25-8

224789-26-8

224785-90-4

Literature: WO2013/75680 A1, ; Page/Page column 17 ;

224789-21-3

224785-90-4

Literature: WO2013/75680 A1, ;

Precursor 3
5308-25-8 224789-21-3 224789-26-8
DownStream 0

224785-90-4	224785-91-5
130018-77-8	224785-87-9
461-06-3	1189685-70-8
224788-34-5	448184-48-3
224785-98-2	1417529-69-1