Udenafil

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Chemical Structure| 268203-93-6 同义名 : 优地那非 ;DA8159
CAS号 : 268203-93-6
货号 : A444987
分子式 : C25H36N6O4S
纯度 : 98%
分子量 : 516.66
MDL号 : MFCD20275557
存储条件:

Pure form Inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Udenafil is a potent, selective and orally active phosphodiesterase type 5 (PDE5) inhibitor[3]. Udenafil is as effective in the treatment of diabetes mellitus-associated ED (Erectile dysfunction) as other PDE5Is[4]. Subcutaneous injection of udenafiltreated ASCs (adipose-derived stem cells) accelerated telogen-to-anagen transition in vivo. Udenafil stimulates ASC motility and increases paracrine growth factor, including cytokine signaling. Udenafil-stimulated secretion of cytokine from ASCs may promote hair growth via the ERK and NFκB pathways[5]. Udenafil has a better renoprotective effect than mannitol against I/R (ischemia-reperfusion) injury and this effect supports more functional improvements[6]. Udenafil inhibited the survival and growth of VEC (vascular endothelial cell) and VSMC (vascular smooth muscle cell) in a concentration-dependent manner over a range of concentrations. At 100 μM, udenafil, inhibited VEC proliferation significantly less than VSMC proliferation, and could significantly induce VEC apoptosis less than VSMC apoptosis[7].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00767598 Pharmacokinetics of Three PDE5... 展开 >>Is Healthy Subjects Genetic Polymorphic CYP3A5 收起 << Phase 1 Completed - -
NCT03430583 - Recruiting December 31, 2020 -
NCT01232010 Renal Insufficiency ... 展开 >> Kidney Diseases Urologic Diseases 收起 << Phase 1 Completed - Korea, Republic of ... 展开 >> Asan Medical Center Seoul, Korea, Republic of 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.94mL

0.39mL

0.19mL

9.68mL

1.94mL

0.97mL

19.36mL

3.87mL

1.94mL

参考文献

[1]Zhao C, Kim SH, et al. Activity of phosphodiesterase type 5 inhibitors in patients with lower urinary tract symptoms due to benign prostatic hyperplasia. BJU Int. 2011 Jun;107(12):1943-7.

[2]Paick JS, Kim SW, et al. The efficacy and safety of udenafil, a new selective phosphodiesterase type 5 inhibitor, in patients with erectile dysfunction. J Sex Med. 2008 Apr;5(4):946-53.

[3]Paick JS, Kim SW, Yang DY, Kim JJ, Lee SW, Ahn TY, Choi HK, Suh JK, Kim SC. The efficacy and safety of udenafil, a new selective phosphodiesterase type 5 inhibitor, in patients with erectile dysfunction. J Sex Med. 2008 Apr;5(4):946-953

[4]Cho MC, Paick JS. Udenafil for the treatment of erectile dysfunction. Ther Clin Risk Manag. 2014 May 14;10:341-54

[5]Choi N, Sung JH. Udenafil Induces the Hair Growth Effect of Adipose-Derived Stem Cells. Biomol Ther (Seoul). 2019 Jul 1;27(4):404-413

[6]Özlülerden Y, Toktaş C, Aybek H, Küçükatay V, Şen Türk N, Zumrutbas AE. The renoprotective effects of mannitol and udenafil in renal ischemia-reperfusion injury model. Investig Clin Urol. 2017 Jul;58(4):289-295

[7]Fang CH, Song YS, So BI, Kim H, Shin JH, Kim KS. Concentration-dependent differential effects of udenafil on viability, proliferation, and apoptosis in vascular endothelial and smooth muscle cells. Indian J Pharmacol. 2014 May-Jun;46(3):292-7