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Avanafil (dibenzenesulfonate)

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Description
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].
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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
PDE1; PDE10; PDE2; PDE4; PDE5; PDE6; PDE7

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