CAS 224785-90-4|Vardenafil

Introduction：Basic information about CAS 224785-90-4|Vardenafil, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Vardenafil BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Articles27
6. Synonyms

Common Name	Vardenafil
CAS Number	224785-90-4	Molecular Weight	488.60
Density	1.4±0.1 g/cm3	Boiling Point	692.2ºC at 760mmHg
Molecular Formula	C₂₃H₃₂N₆O₄S	Melting Point	214-216ºC
MSDS	/	Flash Point	372.5ºC
Symbol	GHS02, GHS07	Signal Word	Danger

Names

Name	vardenafil
Synonym	More Synonyms

Vardenafil BiologicalActivity

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.

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.

Chemical & Physical Properties

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
InChIKey	SECKRCOLJRRGGV-UHFFFAOYSA-N
SMILES	CCCc1nc(C)c2c(=O)[nH]c(-c3cc(S(=O)(=O)N4CCN(CC)CC4)ccc3OCC)nn12
Storage condition	?20°C

Safety Information

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

Articles27

Improvement of exercise capacity in monocrotaline-induced pulmonary hypertension by the phosphodiesterase-5 inhibitor Vardenafil.

Respir. Physiol. Neurobiol. 186(1) , 61-4, (2013)

Vardenafil, a phosphodiesterase-5 inhibitor, is approved for the therapy of erectile dysfunction. However, in contrast to Sildenafil and Tadalafil, little is known about its effects on pulmonary hyper...

SOP conservative (medical and mechanical) treatment of erectile dysfunction.

J. Sex. Med. 10(1) , 130-71, (2013)

Erectile dysfunction (ED) is the most frequently treated male sexual dysfunction worldwide. ED is a chronic condition that exerts a negative impact on male self-esteem and nearly all life domains incl...

High inter-individual variability of vardenafil pharmacokinetics in patients with pulmonary hypertension.

Eur. J. Clin. Pharmacol. 69(2) , 197-207, (2013)

To evaluate the pharmacokinetic parameters of a single oral dose of vardenafil in patients with pulmonary hypertension (PH).Sixteen patients with PH received vardenafil in single oral doses (20, 10 or...

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)

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