Vardenafil HCl Trihydrate

Catalog No.S2515 Synonyms: BAY38-9456

Vardenafil HCl Trihydrate Chemical Structure

Molecular Weight(MW): 579.11

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

Size Price Stock Quantity  
In DMSO USD 120 In stock
USD 90 In stock
USD 570 In stock
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Cited by 4 Publications

2 Customer Reviews

  • (G) Immunoblot analysis for TAZ and Nanog in PCSC after vardenafil treatments. (H) Cytotoxicity to DDP in PCSC treated with indicated concentrations of vardenafil. **p < 0.01, *p < 0.05 versus PC3 cells, vardenafil at 0 μM, or DDP at 0 μM; ++p < 0.01, +p < 0.05 versus vardenafil at 0 μM.

    Cancer Lett, 2016, 378(1):38-50.. Vardenafil HCl Trihydrate purchased from Selleck.

    H&E and immunostaining of FOXM1, ABCC10, Ki-67 and TUNEL in tumor sections are shown (scale bar, 25μm).

    Oncotarget, 2017, 8(5):8574-8589. Vardenafil HCl Trihydrate purchased from Selleck.

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Biological Activity

Description Vardenafil HCl Trihydrate 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

Solubility (25°C)

In vitro DMSO 100 mg/mL (172.67 mM)
Ethanol 20 mg/mL (34.53 mM)
Water 10 mg/mL (17.26 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 579.11
Formula

C23H32N6O4S.HCl.3H2O

CAS No. 330808-88-3
Storage powder
in solvent
Synonyms BAY38-9456

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03102398 Recruiting Erectile Dysfunction Tritech Biopharmaceuticals Co. Ltd.|A2 Healthcare Taiwan Corporation March 31 2017 Phase 1|Phase 2
NCT03102398 Recruiting Erectile Dysfunction Tritech Biopharmaceuticals Co. Ltd.|A2 Healthcare Taiwan Corporation March 31 2017 Phase 1|Phase 2
NCT02344823 Unknown status Cirrhosis|Erectile Dysfunction Medical University of Vienna June 2012 Phase 4
NCT02344823 Unknown status Cirrhosis|Erectile Dysfunction Medical University of Vienna June 2012 Phase 4
NCT02450188 Completed Erectile Dysfunction University of Florence March 2012 Phase 4
NCT02450188 Completed Erectile Dysfunction University of Florence March 2012 Phase 4

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.

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PDE Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID