Chinese Japanese Germany Korea
ChemicalBook >> CAS DataBase List >>5-Pyrimidinecarboxamide, 4-[[(3-chloro-4-methoxyphenyl)methyl]amino]-2-[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-, benzenesulfonate (1:2)

5-Pyrimidinecarboxamide, 4-[[(3-chloro-4-methoxyphenyl)methyl]amino]-2-[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-, benzenesulfonate (1:2)

5-Pyrimidinecarboxamide, 4-[[(3-chloro-4-methoxyphenyl)methyl]amino]-2-[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-, benzenesulfonate (1:2) Structure
5-Pyrimidinecarboxamide, 4-[[(3-chloro-4-methoxyphenyl)methyl]amino]-2-[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-, benzenesulfonate (1:2) structure
CAS No.
330784-48-0
Chemical Name:
5-Pyrimidinecarboxamide, 4-[[(3-chloro-4-methoxyphenyl)methyl]amino]-2-[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-, benzenesulfonate (1:2)
Synonyms
Avanafil dibesylate;Avanafil dibenzenesulfonate;5-Pyrimidinecarboxamide, 4-[[(3-chloro-4-methoxyphenyl)methyl]amino]-2-[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-, benzenesulfonate (1:2)
CBNumber:
CB29959381
Molecular Formula:
C29H32ClN7O6S
Molecular Weight:
642.13
MDL Number:
MOL File:
330784-48-0.mol
MSDS File:
SDS
Last updated:2026-04-21 10:31:43
Request For Quotation

5-Pyrimidinecarboxamide, 4-[[(3-chloro-4-methoxyphenyl)methyl]amino]-2-[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-, benzenesulfonate (1:2) Properties

FDA UNII 4NIU4R914C

5-Pyrimidinecarboxamide, 4-[[(3-chloro-4-methoxyphenyl)methyl]amino]-2-[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-, benzenesulfonate (1:2) Chemical Properties, Uses, Production

Uses

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].

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.

IC 50

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)

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. DOI:10.12659/MSMBR.908504
[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. DOI:10.1016/j.urology.2013.10.021
[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. DOI:10.1016/j.juro.2012.03.115

5-Pyrimidinecarboxamide, 4-[[(3-chloro-4-methoxyphenyl)methyl]amino]-2-[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-, benzenesulfonate (1:2) Preparation Products And Raw materials

Raw materials

Preparation Products

5-Pyrimidinecarboxamide, 4-[[(3-chloro-4-methoxyphenyl)methyl]amino]-2-[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-, benzenesulfonate (1:2) Suppliers

Global Suppliers ( 2)
Supplier Tel Email Country ProdList Advantage
TargetMol Chemicals Inc. 15002134094 marketing@targetmol.cn China 29874 58
TargetMol Chemicals Inc. 13564774135 marketing@targetmol.com United States 19950 58
Supplier Advantage
TargetMol Chemicals Inc. 58
TargetMol Chemicals Inc. 58

View Latest Price from 5-Pyrimidinecarboxamide, 4-[[(3-chloro-4-methoxyphenyl)methyl]amino]-2-[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-, benzenesulfonate (1:2) manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Avanafil dibesylate pictures 2026-04-21 Avanafil dibesylate
330784-48-0
 $1520.00-2500.00 10g TargetMol Chemicals Inc.
5-Pyrimidinecarboxamide, 4-[[(3-chloro-4-methoxyphenyl)methyl]amino]-2-[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-, benzenesulfonate (1:2) Avanafil dibenzenesulfonate Avanafil dibesylate 330784-48-0 C29H32ClN7O6S