2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Autophagy
  3. RAR/RXR Autophagy
  4. Tarenflurbil

Tarenflurbil  (Synonyms: R-氟比洛芬; (R)-Flurbiprofen; MPC7869)

目录号: HY-10291 纯度: 99.96%
COA 产品使用指南

摩尔计算器

Tarenflurbil ((R)-Flurbiprofen) 是 Flurbiprofen 的 R 型对映体，Tarenflurbil 抑制 [3H]9-cis-RA 结合到 RXRα LBD，IC50 为 75 μM。Tarenflurbil 可用于阿尔兹海默症的研究。

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Tarenflurbil Chemical Structure

Tarenflurbil Chemical Structure

CAS No. : 51543-40-9

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10 mM * 1 mL in DMSO ￥605
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Tarenflurbil 相关抗体

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Top Publications Citing Use of Products

    Tarenflurbil purchased from MCE. Usage Cited in: J Appl Toxicol. 2020 Apr;40(4):470-482.  [Abstract]

    The application of 9-cis-RA leads to the degradation of RXRα, restores the activity of NRF2/ARE pathway, and reduces DMF mediated hepatic apoptosis in HL-7702/HuH6 cells. Cells are treated for 48 h with vehicle (DMSO) or with 10 μM 9-cis-RA in the absence or presence of 150 mM DMF. Protein levels are detected by Western blotting.

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Tarenflurbil ((R)-Flurbiprofen) is the R-enantiomer of the racemate NSAID Flurbiprofen, Tarenflurbil ((R)-Flurbiprofen) inhibits the binding of [3H]9-cis-RA to RXRα LBD with IC50 of 75 μM. Tarenflurbil can be used for Alzheimer's disease research.

    IC50 & Target

    IC50: 75 μM (RXRα)[1]
    体外研究
    (In Vitro)

    Tarenflurbil ((R)-Flurbiprofen) can significantly reduce Aβ secretion, but at the same time, increases the level of intracellular Aβ. The binding between [3H]9-cis-RA and RXRα is competitively inhibited by both unlabeled (R)-Flurbiprofen and 9-cis-RA. (R)-Flurbiprofen can interfere with the interaction between RXRα and 9-cis-retinoid acid (9-cis-RA), and that 9-cis-RA decreases Tarenflurbil ((R)-Flurbiprofen)’s reduction of Aβ secretion. Tarenflurbil ((R)-Flurbiprofen) treatment significantly increases the levels of intracellular Aβ species[1]. The well characterized, nonsteroidal anti-inflammatory drug (nonsteroidal anti-inflammatory drug), Tarenflurbil ((R)-Flurbiprofen) affects only Aβ and not Notch β formation, indicating that second generation GSMs and nonsteroidal anti-inflammatory drug-based GSMs have different modes of action regarding Notch processing[2].

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

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

    Effects of the early and late onset of treatment with Tarenflurbil ((R)-Flurbiprofen) are assessed in C57BL6/J mice that develop a non-remitting form of the disease, and in SJL mice that develop a relapsing-remitting (RR)-EAE. Tarenflurbil ((R)-Flurbiprofen) completely prevents the development of clinical EAE scores in C57BL6/J mice when the treatment is started within 3 days after immunization. This regimen is referred to as preventive treatment. The effect is dose-dependent, and the minimum daily dose for complete prevention is 5 mg/kg/day. Effects of Tarenflurbil ((R)-Flurbiprofen) are comparable to those of Fingolimod (FTY720, 0.5 mg/kg/day), which is used as the positive control. Tarenflurbil ((R)-Flurbiprofen) also significantly reduces clinical EAE scores in C57BL6/J mice when treatment is started shortly before onset of clinical manifestations, referred to as semi-therapeutic (10 mg/kg/day) and reduces clinical scores when the treatment is initiated after full development of the disease on day 13 (5 mg/g/day)[3].

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

    244.26

    Formula

    C15H13FO2
    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    R-氟比洛芬；R-氟布洛芬；R-氟吡洛芬；R-氟苯布洛芬；R-苯氟布洛芬
    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
    In Vitro: 

    DMSO 中的溶解度 : ≥ 50 mg/mL (204.70 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)

    * "≥" 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 4.0940 mL 20.4700 mL 40.9400 mL
    5 mM 0.8188 mL 4.0940 mL 8.1880 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

    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 (10.23 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (10.23 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 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

    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: 99.96%

    COA (195 KB) LCMS (266 KB)

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

    HEK293 cells stably expressing human FLAG-Notch1-ΔE (FLAG-NΔE) or APPswe are cultured in Dulbecco's modified Eagle's medium supplemented with 10% fetal bovine serum, nonessential amino acids, 10 μM Hepes, and 300 μg/mL hygromycin or 100 μg/mL Zeocin, respectively. For each experiment, the cells are counted and plated in T75 flasks, 6- or 384-well plates (for Nβ, Aβ, and NICD experiments, respectively) the day before treatment. On the following day, the GSM, Tarenflurbil ((R)-Flurbiprofen) (200 μM), sulindac sulfide (125 μM), AZ1136 (25 μM), AZ4126 (400 nM), or vehicle control (Me2SO) is separately added to fresh cell media and incubated for 24, 16, or 5 h (for Nβ, Aβ, and NICD experiments, respectively) before conditioned media or cells are analyzed[2].

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

    Mice[3]
    Female C57BL6/J and female SJL mice, aged 10-12 weeks at immunization, are used for study of primary progressive EAE and relapsing-remitting EAE, respectively. Mice are housed at 3-5 mice per cage at constant room temperature (21±1°C) under a regular light/dark schedule with light from 7:00 a.m. to 7:00 p.m. Food and water are available ad libitum. Animals are treated orally with Tarenflurbil ((R)-Flurbiprofen), S-Flurbiprofen or vehicle or FTY720 via the drinking water. FTY720 (fingolimod) is used as the positive control at 0.5 mg/kg/day. The therapy is continuous and started on day 3 after immunization for preventive treatment, on day 7-8 to allow for some immune activation for analysis, 4 days before onset of clinical symptoms for semi-therapeutic treatment (C57BL6/J), on day 13 after full development of EAE for late-therapeutic treatment of C57BL6/J mice or after the first peak of the disease 19 days after immunization for late-therapeutic treatment of SJL mice. For late-therapeutic treatment of C57BL6/J mice that have a primary progressive course of the disease and do not recover, ${(R)-Flurbiprofen} or vehicle are administered via drug or vehicle soaked sweet cornflakes to ensure drug, fluid and calories intake during the disease. The animals are accustomed to the cornflakes before the start of the therapy. The evaluation of these different therapeutic paradigms increases the predictability of a potential clinical usefulness of Tarenflurbil ((R)-Flurbiprofen) in human MS. For the"late treatment", mice are allocated pairwise to vehicle and ${(R)-Flurbiprofen} groups according to their clinical scores during the first peak so that the scores are identical in both groups at the onset of treatment. The doses of R-Flurbiprofen are 2.5, 5 and 10 mg/kg in C57BL6/J mice and 5 mg/kg/day for SJL mice. S-Flurbiprofen is used at 10 mg/kg/day. The purity of R- and S-Flurbiprofen is >99.9%, and the stability in drinking water and food is confirmed by LC-MS/MS analyses for up to 7 days at room temperature. After this time, recovery of R-Flurbiprofen is 95.7% and of S-Flurbiprofen 91.5%. The experiments adhered to the guidelines of the Committee for Research and Ethical Issues of the International Association for the Study of Pain (IASP) and to those of GV-SOLAS for animal welfare in science.

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

    Tarenflurbil 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 4.0940 mL 20.4700 mL 40.9400 mL 102.3500 mL
    5 mM 0.8188 mL 4.0940 mL 8.1880 mL 20.4700 mL
    10 mM 0.4094 mL 2.0470 mL 4.0940 mL 10.2350 mL
    15 mM 0.2729 mL 1.3647 mL 2.7293 mL 6.8233 mL
    20 mM 0.2047 mL 1.0235 mL 2.0470 mL 5.1175 mL
    25 mM 0.1638 mL 0.8188 mL 1.6376 mL 4.0940 mL
    30 mM 0.1365 mL 0.6823 mL 1.3647 mL 3.4117 mL
    40 mM 0.1023 mL 0.5117 mL 1.0235 mL 2.5587 mL
    50 mM 0.0819 mL 0.4094 mL 0.8188 mL 2.0470 mL
    60 mM 0.0682 mL 0.3412 mL 0.6823 mL 1.7058 mL
    80 mM 0.0512 mL 0.2559 mL 0.5117 mL 1.2794 mL
    100 mM 0.0409 mL 0.2047 mL 0.4094 mL 1.0235 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:

    Tarenflurbil51543-40-9(R)-Flurbiprofen MPC7869R-氟比洛芬R-氟布洛芬R-氟吡洛芬R-氟苯布洛芬R-苯氟布洛芬MPC7869MPC 7869MPC-7869RAR/RXRAutophagyRetinoic acid receptorsRetinoid X receptorsInhibitorinhibitorinhibit

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