Vardenafil HCl Trihydrate

Catalog No.S2515 Synonyms: BAY38-9456

For research use only.

Vardenafil HCl Trihydrate (BAY38-9456) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.

Vardenafil HCl Trihydrate Chemical Structure

CAS No. 330808-88-3

Selleck's Vardenafil HCl Trihydrate has been cited by 11 Publications

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Biological Activity

Description Vardenafil HCl Trihydrate (BAY38-9456) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.
Targets
PDE5 [1]
(Cell-free assay)
0.7 nM
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. [1] Vardenafil (100 mM) increases cyclic GMP levels in rat hippocampal slices. [2] Vardenafil, tadalafil, and Sildenafil each competitively inhibit cGMP hydrolysis by phosphodiesterase-5 (PDE5), thereby fostering cGMP accumulation and relaxation of vascular smooth muscle. [3]

In vivo Vardenafil dose-dependently potentiates erectile responses to intravenously administered sodium nitroprusside in rabbit. [1] Vardenafil (3 mg/kg, p.o.) results in an improved object discrimination performance in rats. [2] 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. [4] Vardenafil induces powerful preconditioning-like cardioprotective effect against ischemia/reperfusion injury through 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. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 579.11
Formula

C23H32N6O4S.HCl.3H2O

CAS No. 330808-88-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCC1=NC(=C2N1N=C(NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)CC)OCC)C.O.O.O.Cl

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02279992 Terminated Drug: Vardenafil|Drug: Carboplatin Glioma|Brain Neoplasms|Brain Metastasis Cedars-Sinai Medical Center March 27 2012 Early Phase 1
NCT01348880 Completed Drug: Vardenafil ODT (Staxyn BAY38-9456)|Drug: Placebo Erectile Dysfunction Bayer|GlaxoSmithKline|Merck Sharp & Dohme LLC May 2011 Phase 1
NCT01106118 Completed Drug: Vardenafil (Levitra BAY38-9456) Erectile Dysfunction Bayer January 2010 --
NCT01084187 Completed Drug: Vardenafil Erectile Dysfunction|Arterial Hypertension|Endothelial Dysfunction Hospital Universitario Pedro Ernesto January 2010 Phase 4
NCT00738400 Completed Drug: Vardenafil (Levitra BAY38-9456)|Drug: Placebo Erectile Dysfunction|Metabolic Syndrome Bayer November 2008 Phase 4
NCT00718952 Completed Drug: Vardenafil|Drug: Placebo Pulmonary Hypertension Tongji University July 2008 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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