Vardenafil (Vivanza) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively. Vardenafil’s indications and contra-indications are the same as with other PDE5 inhibitors; it is closely related in function to sildenafil citrate (Viagra) and tadalafil (Cialis). Structurally, the difference between the vardenafil molecule and sildenafil citrate is a nitrogen atom’s position and the change of sildenafil’s piperazine ring methyl group to an ethyl group. Chronic vardenafil treatment improves erectile function via structural maintenance of penile corpora cavernosa in rats with acute arteriogenic erectile dysfunction.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 100 mg/mL|
|Related PDE Products|
GLPG1690 is a first-in-class autotaxin (ATX) inhibitor, with IC50 of 131 nM and Ki of 15 nM.
RVT-501 (E6005) is a selective phosphodiesterase 4 (PDE4PDE4) inhibitor with an IC50 of 2.8 nM.
Vardenafil Hcl is a PDE5 inhibitor used for treating erectile dysfunction.
Udenafil(DA8159) is a PDE5 inhibitor used in urology to treat erectile dysfunction.
Theophylline is a methylated xanthine derivative; competitive nonselective phosphodiesterase inhibitor and nonselective adenosine receptor antagonist.
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