Sildenafil

別名：Revatio, UK-92480, Viagra

製品コード：S4684 純度：99.96%

Sildenafil (Revatio, UK-92480, Viagra) is a Phosphodiesterase 5 Inhibitor with IC50 of 5.22 nM.

CAS No. 139755-83-2

サイズ	価格(税別)	在庫状況
100mg	JPY 22000	国内在庫あり
500mg	JPY 44500	国内在庫あり

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

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製品安全説明書

現在のバッチを見る：純度： 99.96%

99.96

Sildenafil関連製品

関連ターゲット	PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE10A PDE9 PDE4B	もっと見る
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関連化合物ライブラリー	Metabolism Compound Library Anti-cancer Metabolism Compound Library Glutamine Metabolism Compound Library Carbohydrate Metabolism Compound Library Lipid Metabolism Compound Library	もっと見る

シグナル伝達経路

PDEシグナル伝達経路

PDE阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Incubation Time	活性情報	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
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生物活性

製品説明

Sildenafil (Revatio, UK-92480, Viagra) is a Phosphodiesterase 5 Inhibitor with IC50 of 5.22 nM.

Targets

PDE5 ^[1]

5.22 nM

In Vitro
In vitro	Sildenafil improves insulin signalling and NO production in endothelial cells, probably by reducing oxidative stress induced by hyperglycemia and by increasing intracellular Ca2+ levels^[2].
細胞実験	細胞株	HUVEC and HAEC
	濃度	1 μM
	反応時間	5 or 72 h
	実験の流れ	HUVEC and HAEC from passages 3 to 6 are cultured for 72 hours in presence of 5.5 mmol/L glucose, 30 mmol/L glucose (high glucose; HG), 10 mmol/L Gluc-N with or without 1 µM of sildenafil (5 or 72 h) and/or 10⁻⁷ M insulin.

In Vivo
In Vivo	Acute administration of the PDE-5 inhibitor sildenafil in a single clinically relevant dose does not modulate the in vivo function of the hypertrophic failing right heart of the rat measured by echocardiography and invasive hemodynamics^[1].
動物実験	動物モデル	Wistar rats
	投与量	1 mg/kg
	投与経路	i.v.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (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
[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

化学情報

分子量	474.58	化学式	C₂₂H₃₀N₆O₄S
CAS No.	139755-83-2	SDF	Download Sildenafil SDFをダウンロードする
Smiles	CCCC1=NN(C2=C1N=C(NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)C)OCC)C
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 50 mg/mL ( (105.35 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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C2=C1/X	C2:	LOG(C2):
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C4=C3/X	C4:	LOG(C4):
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