Avanafil (dibenzenesulfonate)

Avanafil (TA-1790) dibenzenesulfonate is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil dibenzenesulfonate activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil dibenzenesulfonate inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil dibenzenesulfonate can be used for the research of erectile dysfunction and osteoporosis[1][2][3].

Product Specifications

CAS Number

[330784-48-0]

Product Name Alternative

TA1790 (dibenzenesulfonate)

UNSPSC

12352005

Target

Endogenous Metabolite; NO Synthase; Phosphodiesterase (PDE)

Type

Reference compound

Related Pathways

Immunology/Inflammation; Metabolic Enzyme/Protease

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Endocrinology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/avanafil-dibenzenesulfonate.html

Solubility

10 mM in DMSO

Smiles

O=C(C1=CN=C(N2[C@H](CO)CCC2)N=C1NCC3=CC=C(OC)C(Cl)=C3)NCC4=NC=CC=N4.O=S(C5=CC=CC=C5)(O)=O.O=S(C6=CC=CC=C6)(O)=O

Molecular Formula

C35H38ClN7O9S2

Molecular Weight

800.30

References & Citations

[1]Huyut Z, et, al. Effects of the Phosphodiesterase-5 (PDE-5) Inhibitors, Avanafil and Zaprinast, on Bone Remodeling and Oxidative Damage in a Rat Model of Glucocorticoid-Induced Osteoporosis. Med Sci Monit Basic Res. 2018 Mar 13;24:47-58.|[2]Yilmaz D, et, al. The effect of intracavernosal avanafil, a newer phosphodiesterase-5 inhibitor, on neonatal type 2 diabetic rats with erectile dysfunction. Urology. 2014 Feb;83 (2) :508.e7-12. |[3]Kotera J, et, al. Avanafil, a potent and highly selective phosphodiesterase-5 inhibitor for erectile dysfunction. J Urol. 2012 Aug;188 (2) :668-74.