Avanafil dibenzenesulfonate
Based on 1 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- CAS No.: 330784-48-0
- Formula: C35H38ClN7O9S2
- Molecular Weight:800.30
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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Publications Citing Use of MedChemExpress (MCE) Avanafil dibenzenesulfonate
MoreAll Endogenous Metabolite Isoforms
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Biological Activity
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PDE5 5.2 nM (IC50) |
PDE6 630 nM (IC50) |
PDE4 5700 nM (IC50) |
PDE10 6200 nM (IC50) |
PDE7 27000 nM (IC50) |
PDE2 51000 nM (IC50) |
PDE1 53000 nM (IC50) |
Avanafil (TA-1790) dibenzenesulfonate (0.01-1000 µM) enhances by 45% for electrical field stimulation (1-20 Hz)-induced relaxation responses in corpus cavernosum strips from the diabetic group[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Avanafil (TA-1790) dibenzenesulfonate (10 µM; ICI; once, for 10 weeks) improves erectile responses in T2DM rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male rat model of glucocorticoid-induced osteoporosis (GIOP)[1]
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Dosage:10 mg/kg
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Administration:Oral administration; daily, for 30 days
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Result:Decreased the level of eNOS, NO, PDE-5, PICP, MDA, CoQ10/CoQ10H and 8-OHdG/108dG. Increased the level of cGMP, PKG, Cortisol and CTCP.
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Animal Model:Male rat model of glucocorticoid-induced osteoporosis (GIOP)[1]
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Dosage:10 mg/kg
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Administration:Oral administration; daily, for 30 days
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Result:Increased right femur trabecular bone thickness and epiphyseal bone width.
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Animal Model:Male T2DM Sprague Dawley rats[2]
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Dosage:10 µM
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Administration:Intracavernous injection; once, for 10 weeks
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Result:Increased in ICP/MAP in response to nerve stimulation and increased total ICP values.
Chemical Information
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CAS No. 330784-48-0
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Molecular Weight 800.30
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Formula C35H38ClN7O9S2
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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
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Synonyms
TA1790 dibenzenesulfonate
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
Purity & Documentation
References
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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