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Vardenafil

Vardenafil structure

CAS No:
224785-90-4
Formula:
C23H32N6O4S
Chemical Name:
Vardenafil
Synonyms:
Imidazo[5,1-f][1,2,4]triazin-4(1H)-one,2-[2-ethoxy-5-[(4-ethyl-1-piperazinyl)sulfonyl]phenyl]-5-methyl-7-propyl-;Piperazine,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-;2-[2-Ethoxy-5-[(4-ethyl-1-piperazinyl)sulfonyl]phenyl]-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(1H)-one;Vardenafil;2-[2-Ethoxy-5-(4-ethylpiperazin-1-yl-1-sulfonyl)phenyl]-5-methyl-7-propyl-3H-imidazo[5,1-f][1,2,4]triazin-4-one;Nuviva;2-[2-Ethoxy-5-(4-ethyl-piperazine-1-sulfonyl)-phenyl]-5-methyl-7-propyl-imidazo[5,1-f][1,2,4]triazin-4-ol;2-[2-Ethoxy-5-[(4-ethylpiperazin-1-yl)sulfonyl]phenyl]-5-methyl-7-propyl-1H,4H-imidazo[4,3-f][1,2,4]triazin-4-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;Vivanza;1357569-76-6;1437791-28-0
Categories:
Biochemical Engineering > Inhibitors

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 Basic Attributes

Molecular Weight：

579.11

Exact Mass：

488.60

EC Number：

200-835-2

Characteristics

PSA：

121.28000

XLogP3：

2.65

Appearance：

White crystalline powder

Density：

1.4±0.1 g/cm3

Melting Point：

230-235°C

Boiling Point：

692.2ºC at 760mmHg

Flash Point：

9℃

Refractive Index：

1.656

Water Solubility：

3.25e-01 g/L

Storage Conditions：

-20°C

Vapor Pressure：

3.4X10-19 mm Hg at 25 deg C /Estimated/

Safety Information

Transport codes：

UN1230 - class 3 - PG 2 - Methanol, solution

wgk germany：

hazard class code：

11-20/21/22-36

safety instructions：

16-36/37

Marks：

F,Xn

Precautionary statement(s)：

P210-P261-P302 + P352 + P312-P304 + P340 + P312-P337 + P313-P403 + P235

Hazard Statements：

H225-H302 + H312 + H332-H319

Vardenafil Use and Manufacturing

erectil dysfunction;PDE5 inhibitor

Drug Function and Efficacy

By inhibiting the phosphodiesterase type 5 (PDE5) that degrades cGMP in the human corpus cavernosum, the release of local endogenous nitric oxide in the corpus cavernosum under sexual stimulation is increased, thereby enhancing the natural response to sexual stimulation.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Vardenafil Hydrochloride Tablets
Ingredients	Its chemical name is: 2-[2-ethoxy-5-(4-ethyl-piperazine-1-sulfonyl)-phenyl]-5-methyl-7-propyl-3H-imidazole[5,1-f]-[1,2,4]triazine-4-one monohydrochloride.
Indication	CYP inhibitors: Vardenafil is primarily metabolized by the liver enzyme system via cytochrome P450 (CYP) isoenzyme 3A4, with CYP3A5 and CYP2C isoenzymes playing a role in its metabolism. Therefore, inhibitors of these enzymes may reduce the clearance of vardenafil.
Specifications	20 mg

Registered Holders

CHROMO LABORATORIES INDIA PRIVATE LTD

United States
Active
RAKS PHARMA PVT LTD

United States
Active
SMS Pharmaceuticals Ltd

United States
Active

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