Avanafil-13C5

Avanafil-13C5 (TA1790-13C5) is 13C labeled Avanafil. Avanafil (TA-1790) 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 activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis[1][2][3].

TA1790-13C5

12352005

Endogenous Metabolite; Isotope-Labeled Compounds; NO Synthase; Phosphodiesterase (PDE)

Immunology/Inflammation; Metabolic Enzyme/Protease; Others

Metabolism-protein/nucleotide metabolism

Endocrinology; Cardiovascular Disease

COC1=C(Cl)C=C(CNC2=C(C(N[13C][13C]3=N[13C]=[13C][13C]=N3)=O)C=NC(N4[C@H](CO)CCC4)=N2)C=C1

C18 13C5H21ClN7O3

483.87

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[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.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-18252S3/

Isotope-Labeled Compounds

No Development Reported