Vardenafil (hydrochloride trihydrate)

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

Product Specifications

CAS Number

[330808-88-3]

UNSPSC

12352005

Hazard Statement

H301, H373

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

Assay Protocol

https://www.medchemexpress.com/vardenafil-hydrochloride-trihydrate.html

Purity

99.67

Solubility

DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C) |H2O : 100 mg/mL

Smiles

O=C1N=C(C2=CC(S(=O)(N3CCN(CC)CC3)=O)=CC=C2OCC)NN4C1=C(C)N=C4CCC.Cl.O.O.O

Molecular Formula

C23H39ClN6O7S

Molecular Weight

579.11

Precautions

H301, H373

References & Citations

[1]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. |[2]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. |[3]Ahmed N, et al. Hepatoprotective role of vardenafil against experimentally induced hepatitis in mice. J Biochem Mol Toxicol. 2017 Mar. 31 (3) . |[4]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.|[5]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.|[6]Ashour AE, et al. Vardenafil dihydrochloride. Profiles Drug Subst Excip Relat Methodol. 2014;39:515-544.