Sildenafil

别名: Revatio, UK-92480, Viagra 中文名称：西地那非

目录号：S4684 Purity: 99.96%

Sildenafil (Revatio, UK-92480, Viagra) 是Phosphodiesterase 5抑制剂，其IC50为5.22 nM。

Sildenafil Chemical Structure

CAS: 139755-83-2

规格	价格	库存
100mg	795.41	现货
500mg	2433.08	现货
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产品质控

批次：纯度： 99.96%

99.96

Sildenafil相关产品

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细胞实验数据示例

细胞系	实验类型	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

PDE5 ^[1]

5.22 nM

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。

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
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

参考文献
[1] Asger Andersen, et al. Pulmonary Circulation. 2013, 3(3):599-610. [2] Mammi C, et al. PLoS One. 2011, 6(1):e14542.

参考文献

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)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

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

DMSO : 95 mg/mL ( (200.17 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : 3.5 mg/mL (7.37 mM)

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次：

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

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

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）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

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）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

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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操作手册

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* 必填项

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