Avanafil dibenzenesulfonate

Modify Date: 2024-01-09 18:36:12

Avanafil dibenzenesulfonate Structure
Avanafil dibenzenesulfonate structure
Common Name Avanafil dibenzenesulfonate
CAS Number 330784-48-0 Molecular Weight 800.30
Density N/A Boiling Point N/A
Molecular Formula C35H38ClN7O9S2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Avanafil dibenzenesulfonate


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].

 Names

Name Avanafil dibenzenesulfonate

 Avanafil dibenzenesulfonate Biological Activity

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].
Related Catalog
Target

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)

In Vitro 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].
In Vivo Avanafil (TA-1790) dibenzenesulfonate (10 mg/kg; p.o.; daily, for 30 d; male rat) increases angiogenesis in bone tissue via the activation of NO, cGMP and PKG (NO/cGMP/PKG) signaling-pathway and significantly decreases dexamethasone-induced loss in BMD, bone atrophy, and oxidative stress[1]. Avanafil (TA-1790) dibenzenesulfonate (10 µM; ICI; once, for 10 weeks) improves erectile responses in T2DM rats[2]. Animal Model: Male rat model of glucocorticoid-induced osteoporosis (GIOP)[1] Dosage: 10 mg/kg Administration: Oral administration; daily, for 30 days 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. Animal Model: Male rat model of glucocorticoid-induced osteoporosis (GIOP)[1] Dosage: 10 mg/kg Administration: Oral administration; daily, for 30 days Result: Increased right femur trabecular bone thickness and epiphyseal bone width. Animal Model: Male T2DM Sprague Dawley rats[2] Dosage: 10 µM Administration: Intracavernous injection; once, for 10 weeks Result: Increased in ICP/MAP in response to nerve stimulation and increased total ICP values.
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.

[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.

 Chemical & Physical Properties

Molecular Formula C35H38ClN7O9S2
Molecular Weight 800.30