Sildenafil
别名: Revatio, UK-92480, Viagra 中文名称：西地那非
Sildenafil (Revatio, UK-92480, Viagra) 是Phosphodiesterase 5抑制剂，其IC50为5.22 nM。
Sildenafil Chemical Structure
CAS: 139755-83-2
客户使用Selleck的Sildenafil发表文献20篇
客户使用该产品的1个实验数据
产品质控
Sildenafil相关产品
相关信号通路图
PDE抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| human erythrocytes | Function assay | 60 mins | Inhibition of ABCC5 in human erythrocytes assessed as inhibition of ATP-mediated [3H]cGMP uptake in inside-out vesicles after 60 mins by liquid scintillation counting, Ki=1.2 μM | 22380603 | |
| HEK293T | Function assay | 2 hrs | Displacement of [3H]ZM241385 from human AA2AR expressed in HEK293T cells after 2 hrs by liquid scintillation counter, Ki=0.19953μM | 22563707 | |
| HEK293T | 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=4.5μM | 23122865 | |
| BL21-CodonPlus(DE3) | Function assay | 30 mins | Inhibition of human His-tagged PDE5A catalytic domain expressed in Escherichia coli BL21-CodonPlus(DE3) cells using [3H]cAMP or [3H]cGMP as substrate incubated for 30 mins by scintillation counting method, IC50=0.0022μM | 26908025 | |
| Sf9 | Function assay | 15 mins | Inhibition of recombinant human PDE5A1 catalytic domain (535 to 860 residues) expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate incubated for 15 mins by liquid scintillation counting method, IC50=0.0022μM | 26908025 | |
| BL21-CodonPlus(DE3) | Function assay | 30 mins | Inhibition of human His-tagged PDE4B catalytic domain expressed in Escherichia coli BL21-CodonPlus(DE3) cells using [3H]cAMP or [3H]cGMP as substrate incubated for 30 mins by scintillation counting method, IC50=20μM | 26908025 | |
| Sf9 | Function assay | 30 mins | Inhibition of full length recombinant human N-terminal GST-tagged PDE5A1 expressed in baculovirus infected Sf9 cells using cGMP as substrate after 30 mins by HTRF assay, IC50=0.004μM | 27606546 | |
| Sf9 | Function assay | 1 hr | Inhibition of N-terminal GST-tagged full length recombinant human PDE5A1 catalytic domain expressed in Baculovirus infected Sf9 insect cells using FAM-cGMP as substrate after 1 hr by fluorescence polarization assay, IC50=0.00365μM | 29505934 | |
| Sf9 | Function assay | 30 mins | Inhibition of N-terminal GST-tagged human PDE5A1 expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay, IC50=0.00431μM | 31021628 | |
| Sf9 | Function assay | 30 mins | Inhibition of N-terminal GST-tagged human PDE6C expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay, IC50=0.03642μM | 31021628 | |
| Sf9 | Function assay | 30 mins | Inhibition of N-terminal GST-tagged human PDE1 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay, IC50=0.819μM | 31021628 | |
| Sf9 | Function assay | 30 mins | Inhibition of N-terminal GST-tagged human PDE11A4 expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay, IC50=4.93μM | 31021628 | |
| RFL-6 | Function assay | Inhibition of phosphodiesterase 5 in rat fetal lung fibroblast (RFL-6) cells, Ki=0.0018μM | 15771456 | ||
| mammalian cells | Function assay | Inhibition of human Potassium channel HERG expressed in mammalian cells, IC50=3.31131μM | 12873512 | ||
| HEK293 | Function assay | TP_TRANSPORTER: inhibition of 9-(2-phosphonomethoxyethyl)adenine(PMEA) efflux (PMEA: 1 uM) in MRP4-expressing HEK293 cells, IC50=20μM | 12695538 | ||
| CHO | Function assay | Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique, IC50=3.31131μM | 18448342 | ||
| COS7 | Function assay | Inhibition of human recombinant PDE5A1 expressed in COS7 cells, IC50=0.075μM | 18778098 | ||
| Sf9 | Function assay | Inhibition of human PDE5A1 expressed in baculovirus in sf9 cells by PDE Glo phosphodiesterase assay, IC50=0.0056μM | 25801159 | ||
| BL21-CodonPlus | Function assay | Inhibition of recombinant human His6-tagged PDE5A (535 to 786 residues)/PDE6C expressed in Escherichia coli BL21-CodonPlus cells using [3H]cGMP as substrate, Ki=0.025μM | 26908025 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Sildenafil (Revatio, UK-92480, Viagra) 是Phosphodiesterase 5抑制剂，其IC50为5.22 nM。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Sildenafil改善内皮细胞中的胰岛素信号转导以及NO的产生。可能的机制是减少由高血糖症引发的氧化应激反应或增加细胞内钙离子水平[2]。 | |||
|---|---|---|---|---|
| 细胞实验 | 细胞系 | HUVEC和HAEC | ||
| 浓度 | 1 μM | |||
| 孵育时间 | 5或72 h | |||
| 方法 | 选择处于passages 3-6阶段的细胞进行培养，在培养基中有5.5 mmol/L 葡萄糖，30 mmol/L 葡萄糖(high glucose; HG)，10 mmol/L Gluc-N，加入或者不加入1 µM sildenafil及/或10-7 M 胰岛素，孵育5小时或72小时。 |
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| 体内研究(In Vivo) | ||
| 体内研究活性 | 通过超声波心动描记术和有创性血流动力学监测，PDE-5抑制剂sildenafil的急性给药（单次注射，临床相关的剂量）并没有调节大鼠的肥厚性右心衰[1]。 | |
|---|---|---|
| 动物实验 | Animal Models | Wistar大鼠 |
| Dosages | 1 mg/kg | |
| Administration | 静脉注射 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05466695 | Not yet recruiting | Erectile Dysfunction and Neutrophil Lymphocyte Ratio |
Assiut University |
August 1 2022 | Early Phase 1 |
| NCT05275725 | Recruiting | Birth Asphyxia |
Pia Wintermark|Kawempe National Referral Hospital|Saint Francis Memorial Hospital|Walimu|McGill University Health Centre/Research Institute of the McGill University Health Centre |
July 1 2022 | Phase 1 |
| NCT04565925 | Recruiting | Spinal Cord Injuries|Urinary Incontinence |
The University of Texas Medical Branch Galveston |
July 7 2021 | Phase 2 |
| NCT04122105 | Unknown status | Renal Transplant Failure |
University of British Columbia |
April 1 2021 | Not Applicable |
化学信息&溶解度
| 分子量 | 474.58 | 分子式 | C22H30N6O4S |
| CAS号 | 139755-83-2 | SDF | Download Sildenafil SDF |
| Smiles | CCCC1=NN(C2=C1N=C(NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)C)OCC)C | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 50 mg/mL ( (105.35 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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