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Avanafil metabolite M4

CAT: 0804-HY-179550Size: 1 EachDry Ice: NoHazardous: No
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Description
Avanafil metabolite M4 (Compound M-4ii) is a metabolite of Avanafil. 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].
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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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