2. Neuronal Signaling Stem Cell/Wnt
  3. γ-secretase
  4. E 2012

E 2012 是有效的 γ 分泌酶调节剂，不会影响 Notch 加工。E 2012 在胆固醇生物合成的最后一步抑制 3β-羟基固醇 Δ24-还原酶 (DHCR24)。E 2012 旨在通过减少淀粉样蛋白 β-42 减少阿兹海默氏病，并在大鼠多次重复给药后诱发白内障。

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E 2012 Chemical Structure

E 2012 Chemical Structure

CAS No. : 870843-42-8

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Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1320
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5 mg ￥1200
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10 mg ￥1800
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Customer Review

E 2012 相关抗体

Top Publications Citing Use of Products

    E 2012 purchased from MCE. Usage Cited in: Cell Rep. 2015 May 5;11(5):689-96.  [Abstract]

    Western blots performed on soluble protein extracts of neurons following treatment with the indicated compounds. Protein extraction performed at day 90 post-neural induction, after 30 days of drug treatment. DAPT treatment (GSI) increases both total and phosphorylated tau expression in the majority of genotypes, assessed at multiple epitopes. By contrast, E2012 (GSM) reduces total tau expression and its phosphorylation in all genotypes assayed, with particularly pronounced effects in Ts21 neuron

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. E 2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat[1].

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HEK293 IC50
    0.16 μM
    Compound: 3, E2012
    Modulation of gamma-secretase in HEK293 cells expressing guinea pig Swedish mutant SFV-APP695sw assessed as inhibition of amyloid beta-42 production after 16 to 18 hrs by HTRF assay
    Modulation of gamma-secretase in HEK293 cells expressing guinea pig Swedish mutant SFV-APP695sw assessed as inhibition of amyloid beta-42 production after 16 to 18 hrs by HTRF assay
    		[PMID: 24139583]
    HEK293 IC50
    14000 nM
    Compound: 1, E-2012
    Modulation of gamma-secretase-mediated cleavage of human APP Swedish and London mutation expressed in HEK293 cells assessed as reduction of total amyloid beta level after 5 hrs by sandwich immunoassay
    Modulation of gamma-secretase-mediated cleavage of human APP Swedish and London mutation expressed in HEK293 cells assessed as reduction of total amyloid beta level after 5 hrs by sandwich immunoassay
    		[PMID: 22098494]
    HEK293 IC50
    2300 nM
    Compound: 1, E-2012
    Modulation of gamma-secretase-mediated cleavage of human APP Swedish and London mutation expressed in HEK293 cells assessed as inhibition of amyloid beta40 production after 5 hrs by sandwich immunoassay
    Modulation of gamma-secretase-mediated cleavage of human APP Swedish and London mutation expressed in HEK293 cells assessed as inhibition of amyloid beta40 production after 5 hrs by sandwich immunoassay
    		[PMID: 22098494]
    HEK293 IC50
    560 nM
    Compound: E2012
    Modulation of gamma-secretase in HEK293 cells expressing Swedish mutant APP assessed as inhibition of intracellular amyloid beta 40 production after 16 hrs by sandwich ELISA
    Modulation of gamma-secretase in HEK293 cells expressing Swedish mutant APP assessed as inhibition of intracellular amyloid beta 40 production after 16 hrs by sandwich ELISA
    		[PMID: 26142947]
    HEK293 IC50
    64 nM
    Compound: 2
    Modulation of gamma secretase in HEK293 cells transfected with human APP with Swedish and London familial AD mutation assessed as reduction in Abeta42 levels incubated for 5 hrs by sandwich immuno-assay
    Modulation of gamma secretase in HEK293 cells transfected with human APP with Swedish and London familial AD mutation assessed as reduction in Abeta42 levels incubated for 5 hrs by sandwich immuno-assay
    		[PMID: 32786237]
    HEK293 IC50
    64 nM
    Compound: 1, E-2012
    Modulation of gamma-secretase-mediated cleavage of human APP Swedish and London mutation expressed in HEK293 cells assessed as inhibition of amyloid beta42 production after 5 hrs by sandwich immunoassay
    Modulation of gamma-secretase-mediated cleavage of human APP Swedish and London mutation expressed in HEK293 cells assessed as inhibition of amyloid beta42 production after 5 hrs by sandwich immunoassay
    		[PMID: 22098494]
    HEK293 IC50
    64 nM
    Compound: 1
    Inhibition of gamma secretase-mediated amyloid beta42 production in HEK293 cells by sandwich immunoassay
    Inhibition of gamma secretase-mediated amyloid beta42 production in HEK293 cells by sandwich immunoassay
    		[PMID: 21195610]
    HEK293 IC50
    85 nM
    Compound: E2012
    Modulation of gamma-secretase in HEK293 cells expressing Swedish mutant APP assessed as inhibition of intracellular amyloid beta 42 production after 16 hrs by sandwich ELISA
    Modulation of gamma-secretase in HEK293 cells expressing Swedish mutant APP assessed as inhibition of intracellular amyloid beta 42 production after 16 hrs by sandwich ELISA
    		[PMID: 26142947]
    体外研究
    (In Vitro)

    E2012 has concentration-dependent inhibitory effects on cholesterol biosynthesis in primary culture of rat hepatocytes and HepG2 cells with IC50s of 11.0, and 15.1 nM, respectively[1].

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

    E 2012 相关抗体:
    体内研究
    (In Vivo)

    In vivo lenticular concentration of E 2012 after 13-week repeated dose with cataract was well above those where inhibition is observed in vitro. E 2012 induces cataract in the rat by inhibiting DHCR24 at the final step of cholesterol synthesis with associated elevation in desmosterol within the lens, preceded by desmosterol changes that would serve as a predictive safety biomarker for lenticular opacity[2].

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

    419.49

    Formula

    C25H26FN3O2
    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    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 : 50 mg/mL (119.19 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 2.3838 mL 11.9192 mL 23.8385 mL
    5 mM 0.4768 mL 2.3838 mL 4.7677 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    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.5 mg/mL (5.96 mM); 澄清溶液; 超声助溶

      此方案可获得 2.5 mg/mL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% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (5.96 mM); 澄清溶液; 超声助溶

      此方案可获得 2.5 mg/mL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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      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

    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
    参考文献

    E 2012 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 2.3838 mL 11.9192 mL 23.8385 mL 59.5962 mL
    5 mM 0.4768 mL 2.3838 mL 4.7677 mL 11.9192 mL
    10 mM 0.2384 mL 1.1919 mL 2.3838 mL 5.9596 mL
    15 mM 0.1589 mL 0.7946 mL 1.5892 mL 3.9731 mL
    20 mM 0.1192 mL 0.5960 mL 1.1919 mL 2.9798 mL
    25 mM 0.0954 mL 0.4768 mL 0.9535 mL 2.3838 mL
    30 mM 0.0795 mL 0.3973 mL 0.7946 mL 1.9865 mL
    40 mM 0.0596 mL 0.2980 mL 0.5960 mL 1.4899 mL
    50 mM 0.0477 mL 0.2384 mL 0.4768 mL 1.1919 mL
    60 mM 0.0397 mL 0.1987 mL 0.3973 mL 0.9933 mL
    80 mM 0.0298 mL 0.1490 mL 0.2980 mL 0.7450 mL
    100 mM 0.0238 mL 0.1192 mL 0.2384 mL 0.5960 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:

    E 2012870843-42-8E2012E-2012γ-secretaseGamma secretaseInhibitorinhibitorinhibit

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    目录号：
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