Tarenflurbil
Based on 4 publication(s) in Google Scholar
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.
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- Purity: 99.58%
- CAS No.: 51543-40-9
- 화학식: C15H13FO2
- 분자량:244.26
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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- Protocol
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Publications Citing Use of MedChemExpress (MCE) Tarenflurbil
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WB
Biological Activity
IC50: 75 μM (RXRα)[1]
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
300 μM
Compound: 1, Tarenflurbil
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Modulation of gamma-secretase expressed in CHO cells co-expressing polyhistidine-tagged APP695NL I-his with FAD-linked Swedish and London mutation assessed as reduction in amyloid beta42 production after 2 hrs by ELISA
Modulation of gamma-secretase expressed in CHO cells co-expressing polyhistidine-tagged APP695NL I-his with FAD-linked Swedish and London mutation assessed as reduction in amyloid beta42 production after 2 hrs by ELISA
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[PMID: 22061640] |
| CHO | IC50 |
305 μM
Compound: 2
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Modulation of gamma-secretase-mediated cleavage of human APP expressed in CHO cells with human presenilin-1 assessed as inhibition of amyloid beta42 production after 24 hrs by ELISA
Modulation of gamma-secretase-mediated cleavage of human APP expressed in CHO cells with human presenilin-1 assessed as inhibition of amyloid beta42 production after 24 hrs by ELISA
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[PMID: 20503989] |
| RAW264.7 | IC50 |
1.3 μM
Compound: 7a
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Inhibition of COX2-mediated 2-arachidonoylglycerol oxygenation in LPS/IFN-gamma-stimulated mouse RAW264.7 cells assessed as 2-AG to PGE2-G/PGD2-G conversion treated 2 hrs after LPS/IFN-gamma stimulation measured after 6 hrs
Inhibition of COX2-mediated 2-arachidonoylglycerol oxygenation in LPS/IFN-gamma-stimulated mouse RAW264.7 cells assessed as 2-AG to PGE2-G/PGD2-G conversion treated 2 hrs after LPS/IFN-gamma stimulation measured after 6 hrs
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[PMID: 22984634] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 51543-40-9
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Appearance Solid
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분자량 244.26
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화학식 C15H13FO2
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Color White to off-white
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SMILES
O=C(O)[C@H](C)C1=CC=C(C2=CC=CC=C2)C(F)=C1
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Synonyms
(R)-Flurbiprofen; MPC7869
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
Esflurbiprofen exerts a fast-onset antidepressant effect by blocking SERT-nNOS interaction. [Abstract]2025 Oct 9. PMID: 41068287 -
J Phys Chem B
Variation of Activation Volume as an Indicator of the Difference in Clusterization Phenomenon Induced by H-Bonding and F-Π Stacking Interactions in Enantiomers and a Racemate of Flurbiprofen. [Abstract]2024 Apr 25;128(16):4021-4032. PMID: 38608273 -
J Appl Toxicol
Retinoid X receptor α (RXRα)-mediated erythroid-2-related factor-2 (NRF2) inactivation contributes to N,N-dimethylformamide (DMF)-induced oxidative stress in HL-7702 and HuH6 cells. [Abstract]2020 Apr;40(4):470-482. PMID: 31875996
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.
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Biochem Biophys Res Commun
Utility of human induced pluripotent stem cell-derived small intestinal epithelial cells for pharmacokinetic, toxicological, and immunological studies. [Abstract]2024 Jan 15:692:149356. PMID: 38071890
용액&용해도
DMSO : 100 mg/mL (409.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (281 KB)
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SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
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Handling Instructions (2659 KB)
References
[1]. You X, et al. Retinoid X receptor-alpha mediates (R )-flurbiprofen's effect on the levels of Alzheimer's beta-amyloid. J Neurochem. 2009 Oct;111(1):142-9. [Content Brief]
[2]. Wanngren J, et al. Second generation γ-secretase modulators exhibit different modulation of Notch β and Aβ production. J Biol Chem. 2012 Sep 21;287(39):32640-50. [Content Brief]
[3]. Schmitz K, et al. R-flurbiprofen attenuates experimental autoimmune encephalomyelitis in mice. EMBO Mol Med. 2014 Sep 30;6(11):1398-422. [Content Brief]
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 |
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