Vardenafil is a piperazinylsulfonyl pyrimidinone PDE5 inhibitor with the highest in vitro potency and PDE5/PDE6 selectivity ratio of the first-generation PDE5 inhibitors. IC50 for PDE5: ~0.7 nM (vs ~3.5 nM sildenafil). Greater PDE5 selectivity over PDE6 (retinal phosphodiesterase) vs sildenafil reduces photophobia and colour vision adverse events — relevant for dose-escalation and selectivity profiling research. Mechanism identical to other PDE5is: cGMP elevation → smooth muscle relaxation. Half-life similar to sildenafil (~4-5h). Available as orodispersible tablet (Staxyn) — alternative PK profile for absorption research.
Also Known As
Levitra, Bay 38-9456, Staxyn
Compound Class
PDE5 inhibitor — highest PDE5 selectivity among first-gen PDE5i
Molecular Formula
C₂₃H₃₂N₆O₄S
Molecular Weight
488.60 Da
CAS Number
224785-90-4
Half-Life
~4–5 hours
Research Applications
PDE5 Selectivity Research
Vardenafil highest PDE5/PDE6 selectivity among first-gen PDE5i. Reference compound for studying consequences of differential PDE6 inhibition (visual effects). Used in PDE isoform selectivity assays comparing all three first-gen agents.
Erectile Function / Haemodynamic Research
Similar mechanism to sildenafil but greater in vitro PDE5 potency. Dose-response studies in corporal smooth muscle relaxation, penile blood flow, and endothelial nitric oxide pathway research.
Diabetes-Associated ED Research
DM patients have reduced endothelial NO production and PDE5 upregulation — vardenafil efficacy in diabetic ED models compared across PDE5i class. Relevant intersection of vascular and metabolic research.
Orodispersible Formulation / PK Research
Staxyn (orodispersible vardenafil): different absorption profile — higher Cmax, similar AUC vs conventional tablet. Research model for orodispersible drug delivery PK comparison.
Key Research Data
Study
Key Findings
Hellstrom et al. 2003 Urology
Vardenafil in ED across severity: superior IIEF improvement vs placebo, dose-response 5-20mg
Goldstein et al. 2003 Int J Impot Res
Diabetic ED: vardenafil vs placebo — significant IIEF improvement in T1DM and T2DM
Orodispersible comparison
Staxyn vs Levitra PK: higher Cmax with orodispersible, buccal absorption component — formulation research data
Specifications
Format
Oral tablet — 20mg per tablet
Purity
≥99% HPLC
Identity
MS confirmed
Storage
Room temperature
PDE5 potency
IC50 ~0.7 nM — most potent first-gen PDE5i in vitro
FAQ
What is Vardenafil (Levitra)?
Vardenafil (Levitra) is a PDE5 inhibitor — highest PDE5 selectivity among first-gen PDE5i. Vardenafil is a piperazinylsulfonyl pyrimidinone PDE5 inhibitor with the highest in vitro potency and PDE5/PDE6 selectivity ratio of the first-generation PDE5 inhibitors. IC50 for PDE5: ~0.7 nM (vs ~3.5 nM sildenafil). Greater PDE5 selectivity over PDE6 (retin…
How does Vardenafil compare to other PDE5 inhibitors?
Vardenafil highest PDE5/PDE6 selectivity among first-gen PDE5i. Reference compound for studying consequences of differential PDE6 inhibition (visual effects). Used in PDE isoform selectivity assays comparing all three first-gen agents….
What research applications does Vardenafil support?
Similar mechanism to sildenafil but greater in vitro PDE5 potency. Dose-response studies in corporal smooth muscle relaxation, penile blood flow, and endothelial nitric oxide pathway research….
Does QSC ship Vardenafil to the USA?
Yes. QSC ships Vardenafil domestically across the USA and to EU, UK, Canada, and Australia. Every batch carries a Janoshik third-party COA confirming ≥99% HPLC purity and MS identity.
