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Vardenafil dihydrochloride

Catalog No. T4480 CAS 224789-15-5

Synonyms: Levitra, Vardenafil Hydrochloride

Vardenafil dihydrochloride (Levitra) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.

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Vardenafil dihydrochloride Chemical Structure

Vardenafil dihydrochloride, CAS 224789-15-5

Pack Size	Availability	Price/USD
25 mg	Inquiry	$ 46.00
50 mg	Inquiry	$ 84.00
100 mg	Inquiry	$ 153.00
200 mg	Inquiry	$ 270.00
1 mL * 10 mM (in DMSO)	Inquiry	$ 81.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Vardenafil dihydrochloride (Levitra) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.
Targets&IC50	PDE5:0.7 nM (Cell-free), PDE1:180 nM (Cell-free)
In vitro	Vardenafil specifically inhibits the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM (6.6 nM). Vardenafil significantly enhances the SNP-induced relaxation of human trabecular smooth muscle at 3 nM (10 nM). Vardenafil also significantly potentiates both ACh-induced and transmural electrical stimulation-induced relaxation of trabecular smooth muscle. Vardenafil (100 mM) increases cyclic GMP levels in rat hippocampal slices. Vardenafil, tadalafil, and Sildenafil each competitively inhibit cGMP hydrolysis by phosphodiesterase-5 (PDE5), thereby fostering cGMP accumulation and relaxation of vascular smooth muscle.
In vivo	Vardenafil dose-dependently potentiates erectile responses to intravenously administered sodium nitroprusside in rabbit. Vardenafil (3 mg/kg, p.o.) results in an improved object discrimination performance in rats. Vardenafil (30 mg/L, p.o.) increases both iNOS and proliferating cell nuclear antigen expression (SM cell replication) in rats, with normalization of the dynamic infusion cavernosometry drop rate and SM/collagen ratio. Vardenafil induces powerful preconditioning-like cardioprotective effect against ischemia/reperfusion injury through the opening of mitochondrial K(ATP) channels in the heart of rabbit. Vardenafil protects the ischemic myocardium against reperfusion injury through a mechanism dependent on mitochondrial K(ATP) channel opening.

Synonyms	Levitra, Vardenafil Hydrochloride
Molecular Weight	561.52
Formula	C23H34Cl2N6O4S
CAS No.	224789-15-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 10 mg/mL (17.27 mM)

Ethanol: 16 mg/mL (27.6 mM)

DMSO: 93 mg/mL (160.6 mM)

References and Literature

1. Saenz d T I, et al. The phosphodiesterase inhibitory selectivity and the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil[J]. International Journal of Impotence Research, 2001, 13(5):282. 2. Prickaerts J, et al. Effects of two selective phosphodiesterase type 5 inhibitors, sildenafil and vardenafil, on object recognition memory and hippocampal cyclic GMP levels in the rat[J]. Neuroscience, 2002, 113(2):351-361. 3. Blount M A, et al. Binding of tritiated sildenafil, tadalafil, or vardenafil to the phosphodiesterase-5 catalytic site displays potency, specificity, heterogeneity, and cGMP stimulation[J]. Molecular Pharmacology, 2004, 66(1):144-152. 4. Ferrini M G, et al. Vardenafil prevents fibrosis and loss of corporal smooth muscle that occurs after bilateral cavernosal nerve resection in the rat[J]. Urology, 2006, 68(2):429-435. 5. Salloum F N, et al. Sildenafil and Vardenafil but not Nitroglycerin Limit Myocardial Infarction through Opening of Mitochondrial KATP Channels when Administered at Reperfusion following Ischemia in Rabbits[J]. Journal of Molecular & Cellular Cardiology, 2007, 42(2):453-458.

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Keywords

Vardenafil dihydrochloride 224789-15-5 Metabolism PDE cGMP Levitra erectile dysfunction impotence Vardenafil Pharmacokinetics erectile selective zucker diabetic fatty rats inhibit smooth diabetes Inhibitor Endogenous Metabolite hepatitis dysfunction muscle Vardenafil Hydrochloride stimulation Vardenafil Dihydrochloride Phosphodiesterase (PDE) inhibitor

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