Vardenafil

Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4[1]. Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels[2]. Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes[1]-[6].

Product Specifications

CAS Number

[224785-90-4]

UNSPSC

12352005

Hazard Statement

H301, H373, H410

Target

Endogenous Metabolite; Phosphodiesterase (PDE)

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Endocrinology; Metabolic Disease; Inflammation/Immunology; Cancer

Assay Protocol

https://www.medchemexpress.com/Vardenafil.html

Purity

99.81

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

CCCC1=NC(C)=C2N1N=C(C(C=C(S(=O)(N3CCN(CC)CC3)=O)C=C4)=C4OCC)NC2=O

Molecular Formula

C23H32N6O4S

Molecular Weight

488.60

Precautions

H301, H373, H410

References & Citations

[1]Ashour AE, et al. Vardenafil dihydrochloride. Profiles Drug Subst Excip Relat Methodol. 2014;39:515-544.|[2]Saenz de Tejada I, et al. The phosphodiesterase inhibitory selectivity and the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Int J Impot Res. 2001;13 (5) :282-290.|[3]Gresser U, et al. Erectile dysfunction: comparison of efficacy and side effects of the PDE-5 inhibitors sildenafil, vardenafil and tadalafil--review of the literature. Eur J Med Res. 2002 Oct 29. 7 (10) :435-46. |[4]Oudot A, et al. Combination of BAY 60-4552 and vardenafil exerts proerectile facilitator effects in rats with cavernous nerve injury: a proof of concept study for the treatment of phosphodiesterase type 5 inhibitor failure. Eur Urol. 2011 Nov. 60 (5) :1020-6. |[5]Ahmed N, et al. Hepatoprotective role of vardenafil against experimentally induced hepatitis in mice. J Biochem Mol Toxicol. 2017 Mar. 31 (3) . |[6]Bódi B, et al. Long-Term PDE-5A Inhibition Improves Myofilament Function in Left and Right Ventricular Cardiomyocytes through Partially Different Mechanisms in Diabetic Rat Hearts. Antioxidants (Basel) . 2021 Nov 6. 10 (11) :1776.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture and light)

Scientific Category

Reference compound1

Clinical Information

Launched

Isoform

PDE1; PDE3; PDE4; PDE5; PDE6

Citation 01

ACS Environ Au. 2025 Aug 8.|Anal Chem. 2025 Jun 3;97 (21) :11099-11109.|Anim Cells Syst (Seoul) . 2019 May 16;23 (3) :155-163.|Pharmacia. 2025 Jul 3.|Life Sci. 2022 Nov 15:309:120992.