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阿伐那非 /Avanafil {[allProObj[0].p_purity_real_show]}

货号:A803364 同义名: TA1790

Avanafil is a potent and highly selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 of 5.2 nM for erectile dysfunction, exhibiting lower selectivity against PDE1, PDE6, and PDE11.

Avanafil 化学结构 CAS号:330784-47-9
Avanafil 化学结构
CAS号:330784-47-9
Avanafil 3D分子结构
CAS号:330784-47-9
Avanafil 化学结构 CAS号:330784-47-9
Avanafil 3D分子结构 CAS号:330784-47-9
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Avanafil 纯度/质量文件 产品仅供科研

货号:A803364 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 PDE PDE1 PDE10A PDE2 PDE3 PDE4 PDE5 PDE6 其他靶点 纯度
Doxofylline 99+%
Deltarasin +++

PDEδ , Kd: 38 nM

99+%
7-(2,3-Dihydroxypropyl)theophylline 98%
Aminophylline +

PDE, IC50: 0.12 mM

98+%
Anagrelide HCl 99%+
Irsogladine AChR,mAChR 98%
PF-8380 +++

Autotaxin, IC50: 2.8 nM

99%+
Dipyridamole 98%
Balipodect ++++

PDE10A, IC50: 0.3 nM

99%+
PF-2545920 ++++

PDE10A, IC50: 0.37 nM

97%
Luteolin +

PDE1, Ki: 15.0 μM

++

PDE2, Ki: 6.4 μM

+

PDE3, Ki: 13.9 μM

+

PDE4, Ki: 11.1 μM

+

PDE5, Ki: 9.5 μM

98%
Milrinone ++

PDE2, IC50: 5.2 μM

++

PDE3, IC50: 2.1 μM

ATPase 98%
Pimobendan ++

PDE3, IC50: 0.32 μM

98%
Cilostazol ++

PDE3, IC50: 0.2 μM

98%
Fenspiride HCl +

PDE3, pIC50: 3.44

+

PDE4, pIC50: 4.16

98%
(S)-(+)-Rolipram ++

PDE4, IC50: 0.75 μM

98%
Apremilast +++

PDE4, IC50: 74 nM

98%
GSK256066 ++++

PDE4B, IC50: 3.2 pM

98+%
Roflumilast ++++

PDE4A4, IC50: 4.3 nM

PDE4A1, IC50: 0.7 nM

99%
Rolipram +++

PDE4B, IC50: 130 nM

99%+
Cilomilast +++

LPDE4, IC50: 100 nM

HPDE4, IC50: 120 nM

98+%
Avanafil ++++

PDE5, IC50: 1 nM

98%
Vardenafil HCl Trihydrate ++++

PDE5, IC50: 0.7 nM

98%
Tadalafil ++++

PDE5, IC50: 1.8 nM

98%
Icariin ++

PDE5, IC50: 0.432 μM

98%
Sildenafil +++

PDE6, IC50: 33 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Avanafil 生物活性

靶点
  • PDE5

    PDE5, IC50:1 nM

描述 Avanafil (TA-1790) exhibits strong and specific inhibitory effects on phosphodiesterase-5 (PDE-5), with IC50 values being 5.2 nM for PDE-5 and progressively higher for PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2, and PDE-1. It enhances the NO/cGMP/PKG signaling pathway, leading to a reduction in bone mineral density (BMD) loss, bone weakening, and oxidative stress. By preventing the breakdown of cyclic guanosine monophosphate (cGMP), Avanafil elevates cGMP levels, making it a candidate for studies on erectile dysfunction and osteoporosis[1][2][3].
体内研究

Administered orally at 10 mg/kg daily for 30 days to male rats, Avanafil (TA-1790) promotes angiogenesis in bone tissue through the NO/cGMP/PKG pathway and notably reduces the dexamethasone-induced decrease in BMD, bone deterioration, and oxidative stress[1].

体外研究

In corpus cavernosum strips from diabetic subjects, Avanafil (TA-1790) at concentrations ranging from 0.01 to 1000 µM increases the relaxation response induced by electrical field stimulation (1-20 Hz) by 45%[2].

Avanafil 参考文献

[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.

Avanafil 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.07mL

0.41mL

0.21mL

10.33mL

2.07mL

1.03mL

20.66mL

4.13mL

2.07mL

Avanafil 技术信息

CAS号330784-47-9
分子式C23H26ClN7O3
分子量 483.951
别名 TA1790
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 15 mg/mL(30.99 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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