- 抑制劑
- 研究領(lǐng)域
- PI3K/Akt/mTOR信號(hào)通路
- 表觀遺傳
- 甲基化
- 免疫&炎癥
- 酪氨酸蛋白激酶
- 血管生成
- 凋亡
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- JAK/STAT信號(hào)通路
- MAPK信號(hào)通路
- 細(xì)胞骨架
- 細(xì)胞周期
- TGF-beta/Smad信號(hào)通路
- DNA損傷/DNA修復(fù)
- 化合物庫(kù)
- 抗體
- 生物試劑
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實(shí)驗(yàn)
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 細(xì)胞核與細(xì)胞漿蛋白抽提試劑盒
- 免疫磁珠
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲(chǔ)液)
- 磷酸酶抑制劑Cocktail
- 細(xì)胞實(shí)驗(yàn)
- Cell Counting Kit-8 (CCK-8)
- 動(dòng)物實(shí)驗(yàn)
- 鼠尾直接PCR試劑盒(快速基因型鑒定)
- 小鼠CD3+ T細(xì)胞分選試劑盒
- 小鼠CD4+ T細(xì)胞分選試劑盒
- 小鼠CD8+ T細(xì)胞分選試劑盒
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Sildenafil
別名: Revatio, UK-92480, Viagra 中文名稱(chēng)：西地那非
Sildenafil (Revatio, UK-92480, Viagra) 是Phosphodiesterase 5抑制劑，其IC50為5.22 nM。
Sildenafil Chemical Structure
CAS: 139755-83-2
產(chǎn)品質(zhì)控
批次：
純度：
99.96%
99.96
Sildenafil相關(guān)產(chǎn)品
| 相關(guān)靶點(diǎn) | PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE10A PDE9 PDE4B | 點(diǎn)擊展開(kāi) |
|---|---|---|
| 相關(guān)產(chǎn)品 | Rolipram IBMX Cilomilast Mardepodect (PF-2545920) Icariin Deltarasin PF-8380 GSK256066 Ibudilast Enpp-1-IN-1 S-(+)-Rolipram Doxofylline Diosgenin TAK-063 BRL-50481 Ziritaxestat (GLPG1690) | 點(diǎn)擊展開(kāi) |
| 相關(guān)化合物庫(kù) | 代謝化合物庫(kù) 抗癌代謝化合物庫(kù) 谷氨酰胺代謝化合物庫(kù) 糖代謝化合物庫(kù) 脂代謝化合物庫(kù) | 點(diǎn)擊展開(kāi) |
相關(guān)信號(hào)通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類(lèi)型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)信息(PMID) |
|---|---|---|---|---|---|
| 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 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Sildenafil (Revatio, UK-92480, Viagra) 是Phosphodiesterase 5抑制劑，其IC50為5.22 nM。 | ||
|---|---|---|---|
| 靶點(diǎn) |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | Sildenafil改善內(nèi)皮細(xì)胞中的胰島素信號(hào)轉(zhuǎn)導(dǎo)以及NO的產(chǎn)生。可能的機(jī)制是減少由高血糖癥引發(fā)的氧化應(yīng)激反應(yīng)或增加細(xì)胞內(nèi)鈣離子水平[2]。 | |||
|---|---|---|---|---|
| 細(xì)胞實(shí)驗(yàn) | 細(xì)胞系 | HUVEC和HAEC | ||
| 濃度 | 1 μM | |||
| 孵育時(shí)間 | 5或72 h | |||
| 方法 | 選擇處于passages 3-6階段的細(xì)胞進(jìn)行培養(yǎng)，在培養(yǎng)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 胰島素，孵育5小時(shí)或72小時(shí)。 |
|||
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | 通過(guò)超聲波心動(dòng)描記術(shù)和有創(chuàng)性血流動(dòng)力學(xué)監(jiān)測(cè)，PDE-5抑制劑sildenafil的急性給藥（單次注射，臨床相關(guān)的劑量）并沒(méi)有調(diào)節(jié)大鼠的肥厚性右心衰[1]。 | |
|---|---|---|
| 動(dòng)物實(shí)驗(yàn) | Animal Models | Wistar大鼠 |
| Dosages | 1 mg/kg | |
| Administration | 靜脈注射 | |
| 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 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 |
|
化學(xué)信息&溶解度
| 分子量 | 474.58 | 分子式 | C22H30N6O4S |
| CAS號(hào) | 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 | ||
| 儲(chǔ)存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 50 mg/mL ( (105.35 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計(jì)算器 |
|
體內(nèi)溶解配方 現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動(dòng)物體內(nèi)配方計(jì)算器 | |||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）
mg/kg
g
μL
只
第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計(jì)算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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