2. Metabolic Enzyme/Protease Autophagy Apoptosis Anti-infection
  3. Phosphodiesterase (PDE) Autophagy Apoptosis Bacterial
  4. Sildenafil

Sildenafil  (Synonyms: 西地那非; UK-92480)

目录号: HY-15025 纯度: 99.90%
COA 产品使用指南

摩尔计算器

Sildenafil (UK-92480) 是一种有效的磷酸二酯酶 5 (PDE5)抑制剂，IC50 为 5.22 nM。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Sildenafil Chemical Structure

Sildenafil Chemical Structure

CAS No. : 139755-83-2

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥605
In-stock
50 mg ￥550
In-stock
100 mg ￥770
In-stock
200 mg ￥1200
In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Sildenafil:

Sildenafil 相关抗体

Top Publications Citing Use of Products

    Sildenafil purchased from MCE. Usage Cited in: Physiol Rep. 2023 Jan;11(1):e15549.  [Abstract]

    The index of cell proliferation in the lungs is significantly reduced in hypoxic mice that received CL316243, sildenafil, or riociguat compared with hypoxic mice treated with vehicle.

    查看 Phosphodiesterase (PDE) 亚型特异性产品:

    查看所有亚型
    PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.

    IC50 & Target

    PDE5

     

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HEK-293T IC50
    > 100 μM
    Compound: Sildenafil
    Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
    Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
    		[PMID: 23122865]
    HEK-293T IC50
    4.5 μM
    Compound: Sildenafil
    Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
    Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
    		[PMID: 23122865]
    Sf9 IC50
    > 10000 nM
    Compound: Sildenafil
    Inhibition of human PDE2A1 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay
    Inhibition of human PDE2A1 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay
    		[PMID: 31021628]
    Sf9 IC50
    > 10000 nM
    Compound: Sildenafil
    Inhibition of N-terminal GST-tagged human PDE3 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay
    Inhibition of N-terminal GST-tagged human PDE3 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay
    		[PMID: 31021628]
    Sf9 IC50
    > 10000 nM
    Compound: Sildenafil
    Inhibition of N-terminal GST-tagged human PDE4 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay
    Inhibition of N-terminal GST-tagged human PDE4 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay
    		[PMID: 31021628]
    Sf9 IC50
    > 10000 nM
    Compound: Sildenafil
    Inhibition of N-terminal GST-tagged human PDE7 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay
    Inhibition of N-terminal GST-tagged human PDE7 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay
    		[PMID: 31021628]
    Sf9 IC50
    > 10000 nM
    Compound: Sildenafil
    Inhibition of N-terminal GST-tagged full length human PDE8A1 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay
    Inhibition of N-terminal GST-tagged full length human PDE8A1 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay
    		[PMID: 31021628]
    Sf9 IC50
    > 10000 nM
    Compound: Sildenafil
    Inhibition of N-terminal GST-tagged full length human PDE9A2 expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay
    Inhibition of N-terminal GST-tagged full length human PDE9A2 expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay
    		[PMID: 31021628]
    Sf9 IC50
    > 10000 nM
    Compound: Sildenafil
    Inhibition of N-terminal GST-tagged human PDE10A expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay
    Inhibition of N-terminal GST-tagged human PDE10A expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay
    		[PMID: 31021628]
    Sf9 IC50
    2.2 nM
    Compound: CHEMBL192
    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
    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
    		[PMID: 26908025]
    Sf9 IC50
    36.42 nM
    Compound: Sildenafil
    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
    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
    		[PMID: 31021628]
    Sf9 IC50
    4 nM
    Compound: 1
    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
    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
    		[PMID: 27606546]
    Sf9 IC50
    4.31 nM
    Compound: Sildenafil
    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
    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
    		[PMID: 31021628]
    Sf9 IC50
    4930 nM
    Compound: Sildenafil
    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
    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
    		[PMID: 31021628]
    Sf9 IC50
    5.6 nM
    Compound: 1
    Inhibition of human PDE5A1 expressed in baculovirus in sf9 cells by PDE Glo phosphodiesterase assay
    Inhibition of human PDE5A1 expressed in baculovirus in sf9 cells by PDE Glo phosphodiesterase assay
    		[PMID: 25801159]
    Sf9 IC50
    819 nM
    Compound: Sildenafil
    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
    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
    		[PMID: 31021628]
    体外研究
    (In Vitro)

    与单独使用 5-羟色胺刺激相比，用 1 μM Sildenafil 预处理可增强 ERK1/ERK2 的磷酸化，增加 S 期细胞百分比和细胞增殖 (P<0.05)。用 1 μM 枸橼酸 Sildenafil 预处理后进行血清素刺激可使 OD 值急剧增加至 0.33，与单独进行血清素刺激相比有显著差异 (P<0.05)。1 μM Sildenafil 明显增强 5-羟色胺诱导的 ERK1/ERK2 磷酸化上调[2]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Sildenafil 相关抗体:
    体内研究
    (In Vivo)

    在勃起的狗模型中，与载体相比，Sildenafil 显著增加 ICP 和 ICP/BP，但对 BP 没有显著影响[1]。Sildenafil 处理显著减少 TL+-细胞的数量，剂量为 10 mg/kg。在 pMCAo 后 8 天，Sildenafil 处理 (0.5 和/或 10 mg/kg 剂量) 显著减少了被 Iba-1 染色的小胶质细胞/巨噬细胞数量[3]。据报道，在临床前动物模型中，Sildenafil 可通过增加生长因子 (FGF 和 VEGF) 的分泌来减少皮瓣坏死，并且在组织学上显示其对大鼠海绵状神经结构有效[4]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    分子量

    474.58

    Formula

    C22H30N6O4S
    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    西地那非
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 100 mg/mL (210.71 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.1071 mL 10.5356 mL 21.0713 mL
    5 mM 0.4214 mL 2.1071 mL 4.2143 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.27 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.27 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

    以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比； 如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂： 50% PEG300    50% Saline

      Solubility: ≥ 10 mg/mL (21.07 mM); 澄清溶液

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.90%

    COA (288 KB) HNMR (137 KB) RP-HPLC (138 KB) LCMS (234 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [2]

    Cells at approximately 90% confluence are harvested with 0.1% trypsin/0.01% ethylene diamine tetraacetic acid (EDTA) solution and seeded into a 96-well plate at a density of 2×104 cells/well and grown in RPMI-1640 containing 10% FBS for three days, followed by serum starvation for three days. Cells are then incubated for different time with various concentration of serotonin or 1 μM Sildenafil followed by serotonin with or without U0126, as indicated. Control cells are treated in the same way except sterile PBS replaced the drug. After treatment, medium is changed to fresh medium, and cells are incubated with 5 g/L of MTT for four hours. MTT is then dissolved with 150 μL of 10% DMSO for 20 minutes. The optical densities (OD) in the 96-well plates are determined using a microplate reader at 570 nm[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3][4]

    Mice[3]
    Ischemia is induced in C57Bl/6 mice on postnatal (P) day 9 by permanent middle cerebral artery occlusion (pMCAo), and followed by either PBS or Sildenafil intraperitoneal (i.p.) injections. In the first set of experiments, animals are randomly divided into five groups and treated with either PBS or a single dose of Sildenafil citrate (0.5, 2.5, 10, and 15 mg/kg), given intraperitoneally (i.p.) 5 min after pMCAo. In the second set of experiments, animals are randomly divided into three groups and treated with either PBS or a single dose of Sildenafil citrate (0.5 and 10 mg/kg, i.p.) 5 min after pMCAo.
    Rats[4]
    Thirty male Sprague-Dawley rats weighing between 210 and 240 g are used. Rats from all groups are anesthetized with xylazine + ketamine and then a crush injury is created by using a one-minute long vascular clamp to the right sciatic nerve. One day before the procedure, rats from Group 1 are started on a 28-day treatment consisting of a daily dose of 20 mg/kg body weight Sildenafil given orally via nasogastric tube, while the rats from Group 2 are started on an every-other-day dose of 10 mg/kg body weight Sildenafil citrate. Rats from Group 3 did not receive any drugs. Subjects in all 3 groups are fed ad libitum with normal rat chow and tap water. Forty-two days after the nerve damage is created, the rats underwent a static sciatic index (SSI) test, sedation and motor coordination tests, and accelerated rotarod tests. Rats are sacrificed under anesthesia and their sciatic nerves are removed surgically. Histopathologic analyses of the nerves and bone densitometry evaluation of the extremities are then performed.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    Sildenafil 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1071 mL 10.5356 mL 21.0713 mL 52.6782 mL
    5 mM 0.4214 mL 2.1071 mL 4.2143 mL 10.5356 mL
    10 mM 0.2107 mL 1.0536 mL 2.1071 mL 5.2678 mL
    15 mM 0.1405 mL 0.7024 mL 1.4048 mL 3.5119 mL
    20 mM 0.1054 mL 0.5268 mL 1.0536 mL 2.6339 mL
    25 mM 0.0843 mL 0.4214 mL 0.8429 mL 2.1071 mL
    30 mM 0.0702 mL 0.3512 mL 0.7024 mL 1.7559 mL
    40 mM 0.0527 mL 0.2634 mL 0.5268 mL 1.3170 mL
    50 mM 0.0421 mL 0.2107 mL 0.4214 mL 1.0536 mL
    60 mM 0.0351 mL 0.1756 mL 0.3512 mL 0.8780 mL
    80 mM 0.0263 mL 0.1317 mL 0.2634 mL 0.6585 mL
    100 mM 0.0211 mL 0.1054 mL 0.2107 mL 0.5268 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Sildenafil139755-83-2UK-92480西地那非UK92480UK 92480Phosphodiesterase (PDE)AutophagyApoptosisBacterialInhibitorinhibitorinhibit

    您最近查看的产品:

    Your information is safe with us. * Required Fields.

       产品名称：

    		  

    * 需求量：

    * 客户姓名：

    		 

    * Email：

    * 电话：

    		 

    * 公司或机构名称：

       留言给我们：

    Bulk Inquiry

    Inquiry Information

    产品名称：
    Sildenafil
    目录号：
    HY-15025
    需求量：

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

       产品名称：

    		  

    * Lot #：

    * 客户姓名：

    		 

    * Email：

       电话：

    		 

    * 部门：

    * 公司或机构名称：

    		 

       留言给我们：

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.

    嗨！很高兴为您提供帮助！

    尊敬的 MCE 客户您好，
    请您选择所在区域，我们将转接对应客服为您服务！

    热门区域

    A

    B

    C

    F

    G

    H

    J

    L

    N

    Q

    S

    T

    X

    Y

    Z

    热 A B C F G H J L N Q S T X Y Z