Avanafil metabolite M4

Avanafil metabolite M4 (Compound M-4ii) is a metabolite of Avanafil (HY-18252) . Avanafil is a selective Phosphodiesterase-5 (PDE-5) inhibitor with IC50s of 5.2, 630, 5700, 6200, 12000, 27000, 51000 and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cGMP hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis[1][2][3][4].

Product Specifications

CAS Number

[2656442-91-8]

UNSPSC

12352005

Target

Drug Metabolite; Phosphodiesterase (PDE) ; PKG

Related Pathways

Metabolic Enzyme/Protease; Stem Cell/Wnt

Field of Research

Metabolic Disease

Smiles

COC1=CC=C(C=C1Cl)CNC2=NC(N3C[C@@H](C[C@H]3CO)O)=NC=C2C(NCC4=NC=CC=N4)=O

Molecular Formula

C23H26ClN7O4

Molecular Weight

499.95

References & Citations

[1]Kammoun AK, et al. LC-MS/MS determination of avanafil and its metabolites in rat plasma and brain: pharmacokinetic study after oral administration and transdermal film application. RSC Adv. 2020 Mar 4;10 (16) :9407-9413. |[2]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.|[3]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.|[4]Kotera J, et, al. Avanafil, a potent and highly selective phosphodiesterase-5 inhibitor for erectile dysfunction. J Urol. 2012 Aug;188 (2) :668-74.