1. PI3K/Akt/mTOR Autophagy
  2. PTEN Autophagy
  3. VO-Ohpic trihydrate

VO-Ohpic trihydrate 

目录号: HY-13074 纯度: ≥98.0%
COA 产品使用指南

VO-Ohpic trihydrate 是一种高效的 PTEN 抑制剂,IC50 为 46±10 nM。

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VO-Ohpic trihydrate Chemical Structure

VO-Ohpic trihydrate Chemical Structure

CAS No. : 476310-60-8

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10 mM * 1 mL in DMSO ¥660
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1 mg ¥272
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5 mg ¥600
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10 mg ¥920
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50 mg ¥2744
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100 mg ¥4500
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Other Forms of VO-Ohpic trihydrate:

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Top Publications Citing Use of Products
WB

    VO-Ohpic trihydrate purchased from MCE. Usage Cited in: Redox Biol. 2019 Jan;20:390-401.  [Abstract]

    Western analysis of related genes expression in mice with the treatment of TAC, TAC+RES, and TAC+RES+VO-Ophic.

    VO-Ohpic trihydrate purchased from MCE. Usage Cited in: Redox Biol. 2019 Jan;20:390-401.  [Abstract]

    Immunoblotting analysis show that RES treatment markedly inhibited Ang II-induced degradation of PTEN, activation of AKT and mTOR and inactivation of AMPK, but this effect is reversed by VO-OHpic.

    VO-Ohpic trihydrate purchased from MCE. Usage Cited in: Redox Biol. 2019 Jan;20:390-401.  [Abstract]

    Immunoblotting analysis show that RES treatment markedly inhibited Ang II-induced degradation of PTEN, activation of AKT and mTOR and inactivation of AMPK, but this effect is reversed by VO-OHpic.

    VO-Ohpic trihydrate purchased from MCE. Usage Cited in: Stem Cell Res Ther. 2019 Jul 29;10(1):217.  [Abstract]

    Western blot showing the levels of phosphorylated and non-phosphorylated PTEN, AKT, and mTOR proteins before and after VO-OHpic trihydrate treatment.

    VO-Ohpic trihydrate purchased from MCE. Usage Cited in: Mol Vis. 2018 Jul 23;24:485-494.  [Abstract]

    The miR-21 inhibitor promotes the expression of the PTEN protein and inhibits the expression of p-AKT, and VO-Ohpic trihydrate reverses the effect.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    VO-Ohpic trihydrate is a highly potent inhibitor of PTEN with an IC50 of 46±10 nM.

    IC50 & Target

    IC50: 46±10 nM (PTEN)[1]

    体外研究
    (In Vitro)

    VO-OHpic with two OHpic ligands and an oxo ligand is a sterically demanding molecule, and one will therefore expect that binds substrate will affect the subsequent binding of the inhibitor due to steric hindrance. VO-OHpic significantly inhibits PTEN activity in low nanomolar concentrations (IC50, 46±10 nM), which is in agreement with the previously determined potency (IC50, 35±2 nM) in a PIP3-based assay. The inhibition constants Kic and Kiu are determined to be 27±6 and 45±11 nM, respectively[1]. VO-OHpic is an encouragingly specific and potent PTEN inhibitor. VO-OHpic is the most potent inhibitor (IC50=35 nM) of the PTEN lipid phosphatase activity[2].

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

    体内研究
    (In Vivo)

    PTEN is inhibited in mice by intra-peritoneal injection of VO-OHpic (10 μg/kg) 30 min before ischemia and then exposed them to 30 min of ischemia and 120 min of reperfusion. At the end of the experiment, myocardial infarct size is measured by triphenyltetrazolium chloride (TTC). Myocardial infarct size is significantly decreased in VO-treated mice (25±6 vs. 56±5 %, n=7, P<0.01). There is no difference in the area at risk between these two groups (46±3 vs. 57±3 %, n=7, P>0.05)[3].

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

    分子量

    415.20

    Formula

    C12H16N2O11V

    CAS 号
    性状

    固体

    颜色

    Light green to green

    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 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 50 mg/mL (120.42 mM; 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)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.4085 mL 12.0424 mL 24.0848 mL
    5 mM 0.4817 mL 2.4085 mL 4.8170 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, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1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

    In Vivo:

    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 (6.02 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。

      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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.02 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。

      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 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    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

    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
    参考文献
    Kinase Assay
    [1]

    VO-OHpic is dissolved in DMSO (100 μM) and diluted further to the required concentration with 1% DMSO. For inhibition studies, PTEN is preincubated with VO-OHpic at RT for 10 min before substrate is added to initialise the reaction. Background absorbance (malachite green assay) and fluorescence (OMFP assay) are determined with VO-OHpic in assay buffer and corrected in the data analysis[1].

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

    Animal Administration
    [3]

    Mice[3]
    The experiment is performed with male C57BL6 mice. Briefly, mice are anesthetized with pentobarbital (70 mg/kg). The left coronary artery is occluded about 1-2 mm below the left auricle. Reperfusion is accomplished by loosening the ligature. The PTEN inhibitor VO-OHpic is administered by intra-peritoneal injection at the dosage of 10 μg/kg once 30 min before ischemia. Saline is used as control. At the end of the experiment, the animals are euthanized by transecting the aorta and removing the heart for infarct size determination.

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

    参考文献

    VO-Ohpic trihydrate 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, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1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 2.4085 mL 12.0424 mL 24.0848 mL 60.2119 mL
    5 mM 0.4817 mL 2.4085 mL 4.8170 mL 12.0424 mL
    10 mM 0.2408 mL 1.2042 mL 2.4085 mL 6.0212 mL
    15 mM 0.1606 mL 0.8028 mL 1.6057 mL 4.0141 mL
    20 mM 0.1204 mL 0.6021 mL 1.2042 mL 3.0106 mL
    25 mM 0.0963 mL 0.4817 mL 0.9634 mL 2.4085 mL
    30 mM 0.0803 mL 0.4014 mL 0.8028 mL 2.0071 mL
    40 mM 0.0602 mL 0.3011 mL 0.6021 mL 1.5053 mL
    50 mM 0.0482 mL 0.2408 mL 0.4817 mL 1.2042 mL
    60 mM 0.0401 mL 0.2007 mL 0.4014 mL 1.0035 mL
    80 mM 0.0301 mL 0.1505 mL 0.3011 mL 0.7526 mL
    100 mM 0.0241 mL 0.1204 mL 0.2408 mL 0.6021 mL
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      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.

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