Home Metabolism PDE inhibitor Vardenafil HCl Trihydrate For research use only.

Vardenafil HCl Trihydrate

Synonyms: BAY38-9456

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

Vardenafil HCl Trihydrate Chemical Structure

CAS No. 330808-88-3

Purity & Quality Control

Vardenafil HCl Trihydrate Related Products

Signaling Pathway

PDE Signaling Pathways

PDE Signaling Pathway

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

Chemical Information & Solubility

Molecular Weight 579.11 Formula

C23H32N6O4S.HCl.3H2O
CAS No. 330808-88-3 SDF Download Vardenafil HCl Trihydrate SDF
Smiles CCCC1=NC(=C2N1N=C(NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)CC)OCC)C.O.O.O.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (172.67 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : 10 mg/mL


Molecular Weight Calculator

In vivo
Batch:

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In vivo Formulation Calculator

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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.
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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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