2. Neuronal Signaling Stem Cell/Wnt
  3. Notch γ-secretase
  4. YO-01027

YO-01027  (Synonyms: Dibenzazepine; DBZ)

目录号: HY-13526 纯度: 99.94% ee.: 100.00%
COA 产品使用指南

摩尔计算器

YO-01027 (Dibenzazepine; DBZ) 是高效的 γ-分泌酶抑制剂，裂解 Notch 和 APPL 的 IC50 分别为 2.92 和 2.64 nM。

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YO-01027 Chemical Structure

YO-01027 Chemical Structure

CAS No. : 209984-56-5

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     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 ￥999
In-stock
1 mg ￥490
In-stock
2 mg ￥744
In-stock
5 mg ￥980
In-stock
10 mg ￥1600
In-stock
25 mg ￥3038
In-stock
50 mg ￥4555
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of YO-01027:

YO-01027 相关抗体

Top Publications Citing Use of Products

    YO-01027 purchased from MCE. Usage Cited in: J Clin Invest. 2020 Feb 3;130(2):612-624.  [Abstract]

    Immunoblotting of the indicated proteins in PC9GR cells treated with vehicle (DMSO), DBZ (250 nM) or gefitinib (1 μM). This is a representative image of three different experiments.

    YO-01027 purchased from MCE. Usage Cited in: J Clin Invest. 2020 Feb 3;130(2):612-624.  [Abstract]

    Immunoblotting of the indicated proteins in CHO cells transfected with pBabe empty vector or pEGFRT790M/L858R and treated with vehicle (DMSO) or DBZ (250 nM) and/or gefitinib (1 μM). This is a representative image of two different experiments.

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    YO-01027 (Dibenzazepine;DBZ) is a potent γ-secretase inhibitor with IC50 values of 2.92 and 2.64 nM for Notch and APPL cleavage, respectively.

    IC50 & Target

    IC50: 2.92±0.22 (Notch), 2.64±0.30 (APPL) nM[1]
    体外研究
    (In Vitro)

    Increasing concentrations of DBZ administered to APPL- or Notch-expressing cells leads to the progressive accumulation of APPL CTF fragments and a decrease in NICD production in a strictly dose-dependent manner[1]. The molecular targets of CE and DBZ are the N-terminal fragment of presenilin 1 within the γ-secretase complex[2].

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

    YO-01027 相关抗体:
    体内研究
    (In Vivo)

    DBZ blocks activated Notch1 signaling in abdominal aortic aneurysm (AAA) tissue from both Ang II-infused Apo E-/- mice and human undergoing AAA repair. DBZ markedly prevents Ang II-stimulated accumulation of macrophages and CD4+ T cells, and ERK-mediated angiogenesis, simultaneously reverses Th2 response, in vivo[3]. Administration of DBZ markedly attenuates renal fibrosis and expression of fibrotic markers, including collagen 1α1/3α1, fibronectin, and α-smoothmuscle actin. DBZ significantly inhibits ureteral obstruction -induced expression of transforming growth factor (TGF)- β, phosphorylated Smad 2, and Smad 3[4].

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

    463.48

    Formula

    C26H23F2N3O3
    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    二苯并氮卓
    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 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 71.43 mg/mL (154.12 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)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.1576 mL 10.7880 mL 21.5759 mL
    5 mM 0.4315 mL 2.1576 mL 4.3152 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 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    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.39 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。

    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: 99.94% ee.: 100.00%

    COA (197 KB) HNMR (207 KB) CNMR (137 KB) RP-HPLC (208 KB) NP-HPLC (497 KB) LCMS (87 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [1]

    DBZ (0.1, 1, 2.5, 5, 7.5, 10, 25, 50, 100, 250 nM) are added to the S2 cell medium upon induction of Notch or APPL expression, 6 h before protein harvesting. For each sample, the same inhibitor is also included at the corresponding concentration in the lysis buffer for protein extraction and immunoblot analysis[1].

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

    Mice: Male wild-type (WT) C57BL/6J and Apo E-/- mice are used in the study. Ang II-treated mice are received an intraperitoneal injection of either saline vehicle or γ-secretase inhibitor, dibenzazepine (DBZ) (1 mg/kg/d, dissolved in saline) 1 day before mini-pump implantation, and the treatment continued daily for 4 weeks. The blood pressure is measured in conscious mice using a computerized tail-cuff system. All mice are anesthetized. The aortic tissues are removed and prepared for further histological and molecular analysis[3].

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

    YO-01027 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1576 mL 10.7880 mL 21.5759 mL 53.9398 mL
    5 mM 0.4315 mL 2.1576 mL 4.3152 mL 10.7880 mL
    10 mM 0.2158 mL 1.0788 mL 2.1576 mL 5.3940 mL
    15 mM 0.1438 mL 0.7192 mL 1.4384 mL 3.5960 mL
    20 mM 0.1079 mL 0.5394 mL 1.0788 mL 2.6970 mL
    25 mM 0.0863 mL 0.4315 mL 0.8630 mL 2.1576 mL
    30 mM 0.0719 mL 0.3596 mL 0.7192 mL 1.7980 mL
    40 mM 0.0539 mL 0.2697 mL 0.5394 mL 1.3485 mL
    50 mM 0.0432 mL 0.2158 mL 0.4315 mL 1.0788 mL
    60 mM 0.0360 mL 0.1798 mL 0.3596 mL 0.8990 mL
    80 mM 0.0270 mL 0.1348 mL 0.2697 mL 0.6742 mL
    100 mM 0.0216 mL 0.1079 mL 0.2158 mL 0.5394 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:

    YO-01027209984-56-5Dibenzazepine DBZ二苯并氮卓YO01027YO 01027Notchγ-secretaseGamma secretaseInhibitorinhibitorinhibit

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