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

Tarenflurbil  (Synonyms: (R)-Flurbiprofen; MPC7869)

Cat. No.: HY-10291 Purity: 99.96%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Tarenflurbil Chemical Structure

Tarenflurbil Chemical Structure

CAS No. : 51543-40-9

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
100 mg USD 60 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Tarenflurbil:

Top Publications Citing Use of Products

    Tarenflurbil purchased from MedChemExpress. 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.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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]

    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].

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

    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].

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

    Clinical Trial
    Molecular Weight

    244.26

    Formula

    C15H13FO2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)[C@H](C)C1=CC=C(C2=CC=CC=C2)C(F)=C1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (204.70 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (10.23 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (10.23 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.96%

    References
    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.

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 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
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    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.

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

     

    Salutation

    Applicant Name *

     

    Email Address *

    Phone Number *

     

    Organization Name *

    Department *

     

    Requested quantity *

    Country or Region *

         

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Tarenflurbil
    Cat. No.:
    HY-10291
    Quantity:
    MCE Japan Authorized Agent: