货号:A504277
同义名:
UK-92480;Revatio
Sildenafil, one of the selective phosphodiesterase-5 (PDE5) inhibitors (IC50= 5.22 nM), is considered the best treatment for erectile dysfunction.
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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 | ✔ | 99%+ | |||||||||||||||||
Aminophylline |
+
PDE, IC50: 0.12 mM |
99%+ | |||||||||||||||||
Anagrelide HCl | ✔ | 99%+ | |||||||||||||||||
Irsogladine | ✔ | mAChR,AChR | 99%+ | ||||||||||||||||
PF-8380 |
+++
Autotaxin, IC50: 2.8 nM |
99%+ | |||||||||||||||||
Dipyridamole | ✔ | 99%+ | |||||||||||||||||
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 | 99%+ | |||||||||||||||
Pimobendan |
++
PDE3, IC50: 0.32 μM |
99%+ | |||||||||||||||||
Cilostazol |
++
PDE3, IC50: 0.2 μM |
99%+ | |||||||||||||||||
Fenspiride HCl |
+
PDE3, pIC50: 3.44 |
+
PDE4, pIC50: 4.16 |
99%+ | ||||||||||||||||
(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 |
99%+ | |||||||||||||||||
Vardenafil HCl Trihydrate |
++++
PDE5, IC50: 0.7 nM |
99%+ | |||||||||||||||||
Tadalafil |
++++
PDE5, IC50: 1.8 nM |
98% | |||||||||||||||||
Icariin |
++
PDE5, IC50: 0.432 μM |
98% | |||||||||||||||||
Sildenafil | ✔ |
+++
PDE6, IC50: 33 nM |
99%+ | ||||||||||||||||
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 | Pre-treatment with 1 μM Sildenafil enhances the phosphorylation of ERK1/ERK2, increases the percentage of cells in S phase, and promotes cell proliferation compared to serotonin stimulation alone (P<0.05). Additionally, pretreatment with 1 μM Sildenafil citrate followed by serotonin stimulation significantly increases the OD value to 0.33, which is significantly different from serotonin stimulation alone (P<0.05). Moreover, 1 μM Sildenafil markedly enhances the upregulation of ERK1/ERK2 phosphorylation induced by serotonin[2]. |
体内研究 | In the dog model of erection, Sildenafil citrate significantly increases ICP and ICP/BP but has no significant effect on BP compared to vehicle[1]. Sildenafil treatment significantly reduces the number of TL+-cells at 10 mg/kg but not at 0.5 mg/kg. Additionally, 8 days after pMCAo, Sildenafil treatment (0.5 and/or 10 mg/kg dose) significantly reduces the number of microglia/macrophages stained by Iba-1[3]. Sildenafil citrate has been reported to decrease flap necrosis in preclinical animal models by increasing the secretion of growth factors (FGF and VEGF). Histologically, it is shown to be effective in rat cavernous nerve architecture[4]. |
体外研究 | Pre-treatment with 1 μM Sildenafil enhances the phosphorylation of ERK1/ERK2, increases the percentage of cells in S phase, and promotes cell proliferation compared to serotonin stimulation alone (P<0.05). Additionally, pretreatment with 1 μM Sildenafil citrate followed by serotonin stimulation significantly increases the OD value to 0.33, which is significantly different from serotonin stimulation alone (P<0.05). Moreover, 1 μM Sildenafil markedly enhances the upregulation of ERK1/ERK2 phosphorylation induced by serotonin[2]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
CHO cells | Function assay | Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique, IC50=3.31131 μM | 18448342 | ||
COS7 cells | Function assay | Inhibition of human recombinant PDE5A1 expressed in COS7 cells, IC50=0.075 μM | 18778098 | ||
HEK293T cells | Function assay | 2 h | Displacement of [3H]ZM241385 from human AA2AR expressed in HEK293T cells after 2 hrs by liquid scintillation counter, Ki=0.19953 μM | 22563707 | |
HEK293T cells | Function assay | 45 mins | Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis, IC50=4.5 μM | 23122865 | |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT02372487 | Pregnancy Complication | Not Applicable | Unknown | June 2016 | Egypt ... 展开 >> Menoufia University Recruiting Shebin Elkom, Egypt Contact: tarek elsayed 00201222739097 Contact: mohamed maher Principal Investigator: tarek sayed Saudi Arabia Alhayah national hospital Recruiting Abha, Saudi Arabia Contact: mohamed maher +966558198655 Contact: tarek sayyed Principal Investigator: mohamed maher Alhayah national hospital Recruiting Abha, Saudi Arabia Contact: mohamed maher +966558198655 Principal Investigator: mohamed maher 收起 << |
NCT02524184 | Obesity | Phase 4 | Unknown | September 2016 | China, Hubei ... 展开 >> Wuhan General Hospital Recruiting Wuhan, Hubei, China, 430070 Contact: Guangda Xiang, MD 13517275283 Guangda64@hotmail.com Contact: Lin Xiang, MD 18627838901 xianglin832010@hotmail.com 收起 << |
NCT01800292 | Hypertension, Pulmonary Artery... 展开 >> Ventricular Dysfunction, Left 收起 << | Phase 4 | Completed | - | United States, Arizona ... 展开 >> University of Arizona Medical Center Tucson, Arizona, United States, 85724 收起 << |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.11mL 0.42mL 0.21mL |
10.54mL 2.11mL 1.05mL |
21.07mL 4.21mL 2.11mL |
CAS号 | 139755-83-2 |
分子式 | C22H30N6O4S |
分子量 | 474.57 |
别名 | UK-92480;Revatio;Viagra |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 30 mg/mL(63.21 mM),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 |