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.
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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。 |
靶点 |
|
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]. |
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 |
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 |