Elafibranor
Based on 16 publication(s) in Google Scholar
Elafibranor (GFT505) is a PPARα/δ agonist with EC50s of 45 and 175 nM, respectively. Elafibranor can be used for the study of primary biliary cholangitis.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.66%
- No. CAS: 923978-27-2
- Fòrmula: C22H24O4S
- Peso molecular:384.49
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Publications Citing Use of MedChemExpress (MCE) Elafibranor
More- Acta Pharm Sin B. 2025 Dec;15(12):6382-6398. [Abstract]
- Biomaterials. 2022 Nov:290:121817. [Abstract]
- Biomaterials. 2021 Sep:276:121006. [Abstract]
- Acta Biomater. 2021 Oct 15:134:228-239. [Abstract]
- Eur J Med Chem. 2021 Dec 5:225:113807. [Abstract]
- World J Gastroenterol. 2024 Jul 28;30(28):3428-3446. [Abstract]
- Cells. 2020 Apr 14;9(4):964. [Abstract]
- Int J Mol Sci. 2019 Apr 2;20(7). pii: E1629. [Abstract]
- Bioorg Chem. 2026 Jul 5:175:109764. [Abstract]
- Hepatol Commun. 2020 Nov 29;5(2):217-233. [Abstract]
- iScience. 2025 Apr 3;28(5):112344. [Abstract]
- Sci Rep. 2023 Oct 9;13(1):17019. [Abstract]
- Mol Pharmacol. 2018 Jun;93(6):563-574. [Abstract]
- PLoS One. 2020 Dec 16;15(12):e0243911. [Abstract]
- Pompeu Fabra University. 2026.
- SSRN. 2024 May 30.
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Actividad biológica
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PPAR-α 45 nM (EC50) |
PPAR-δ 175 nM (EC50) |
Elafibranor (GFT505) is being developed as a dual PPAR-α/PPAR-δ agonist for the inhibition of T2DM and non-alcoholic fatty liver disease. Elafibranor has an active metabolite, GFT1007, and both have potent agonist activity for PPAR-α and to a lesser extent for PPAR-δ[1].
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
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 923978-27-2
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Appearance Solid
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Peso molecular 384.49
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Fòrmula C22H24O4S
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Color Light yellow to yellow
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SMILES
CC(C)(OC1=C(C)C=C(/C=C/C(C2=CC=C(SC)C=C2)=O)C=C1C)C(O)=O
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Synonyms
GFT505
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (16)
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Journal Impact Factor
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Most Recent
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Acta Pharm Sin B
2025 Dec;15(12):6382-6398. PMID: 41477334 -
Biomaterials
2022 Nov:290:121817. PMID: 36208587
Elafibranor purchased from MedChemExpress. Usage Cited in: Biomaterials. 2022 Nov:290:121817. [Abstract]
Elafibranor (30 μM; 10 d) prevented FFA-induced lipid uptake of NAFLD MCLS.
Elafibranor purchased from MedChemExpress. Usage Cited in: Biomaterials. 2022 Nov:290:121817. [Abstract]
Elafibranor (30 μM; 48 h) significantly reduced the protein expression levels of Collagen 1 of NAFLD MCLS in the NASH conditions.
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Biomaterials
A fully defined matrix to support a pluripotent stem cell derived multi-cell-liver steatohepatitis and fibrosis model. [Abstract]2021 Sep:276:121006. PMID: 34304139
Elafibranor purchased from MedChemExpress. Usage Cited in: Biomaterials. 2021 Sep:276:121006. [Abstract]
Elafibranor (ELN) (30 μM; 3 d) reduced BODIPY® staining in hEPSC HepMat co-cultures co-treated with OA.
Elafibranor purchased from MedChemExpress. Usage Cited in: Biomaterials. 2021 Sep:276:121006. [Abstract]
Relative expression of fibrogenic and proinflammatory marker genes, and secreted pro-collagen, TNF-α, IL1α, and IL6 in d32 hESC-derived HepMat co-cultures was assessed. Elafibranor (ELN) (30 μM; 3–7 d) decreased COL1A1, COL3A1, and COL5A2 levels in hEPSC HepMat co-cultures.
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Acta Biomater
2021 Oct 15:134:228-239. PMID: 34265474
Elafibranor purchased from MedChemExpress. Usage Cited in: Acta Biomater. 2021 Oct 15:134:228-239. [Abstract]
Elafibranor (ELA) (10-30 μM) could prevent the formation of lipid droplets in on-chip NAFLD.
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Eur J Med Chem
Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome. [Abstract]2021 Dec 5:225:113807. PMID: 34455359 -
World J Gastroenterol
Effects of elafibranor on liver fibrosis and gut barrier function in a mouse model of alcohol-associated liver disease. [Abstract]2024 Jul 28;30(28):3428-3446. PMID: 39091710 -
Cells
2020 Apr 14;9(4):964. PMID: 32295224 -
Int J Mol Sci
2019 Apr 2;20(7). pii: E1629. PMID: 30986904 -
Bioorg Chem
Discovery of Tetrazolone derivatives as potent PPARα/δ dual agonists for metabolic dysfunction-associated steatohepatitis. [Abstract]2026 Jul 5:175:109764. PMID: 41880786 -
Hepatol Commun
2020 Nov 29;5(2):217-233. PMID: 33553970 -
iScience
2025 Apr 3;28(5):112344. PMID: 40276762 -
Sci Rep
A model of hepatic steatosis with declined viability and function in a liver-organ-on-a-chip. [Abstract]2023 Oct 9;13(1):17019. PMID: 37813918 -
Mol Pharmacol
Leflunomide Increases Hepatic Exposure to Methotrexate and Its Metabolite by Differentially Regulating Multidrug Resistance-Associated Protein Mrp2/3/4 Transporters via Peroxisome Proliferator-Activated Receptor α Activation. [Abstract]2018 Jun;93(6):563-574. PMID: 29618584 -
PLoS One
The pharmacodynamic and differential gene expression analysis of PPAR α/δ agonist GFT505 in CDAHFD-induced NASH model. [Abstract]2020 Dec 16;15(12):e0243911. PMID: 33326461 -
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Solvente y solubilidad
DMSO : ≥ 33 mg/mL (85.83 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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 90% (20% SBE-β-CD in Saline)
Solubility: 2.17 mg/mL (5.64 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.17 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Liu ZM, et al. Early investigational drugs targeting PPAR-α for the treatment of metabolic disease.Expert Opin Investig Drugs. 2015 May;24(5):611-21. [Content Brief]
[2]. Ratziu V, et al. Elafibranor, an Agonist of the Peroxisome Proliferator-Activated Receptor-α and -δ, Induces Resolution of Nonalcoholic Steatohepatitis Without Fibrosis Worsening. Gastroenterology. 2016 May;150(5):1147-1159. [Content Brief]
[3]. Hanf R, et al. The dual peroxisome proliferator-activated receptor alpha/delta agonist GFT505 exerts anti-diabetic effects in db/db mice without peroxisome proliferator-activated receptor gamma-associated adverse cardiac effects.Diab Vasc Dis Res. 2014 No [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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6008 mL | 13.0042 mL | 26.0085 mL | 65.0212 mL |
| 5 mM | 0.5202 mL | 2.6008 mL | 5.2017 mL | 13.0042 mL | |
| 10 mM | 0.2601 mL | 1.3004 mL | 2.6008 mL | 6.5021 mL | |
| 15 mM | 0.1734 mL | 0.8669 mL | 1.7339 mL | 4.3347 mL | |
| 20 mM | 0.1300 mL | 0.6502 mL | 1.3004 mL | 3.2511 mL | |
| 25 mM | 0.1040 mL | 0.5202 mL | 1.0403 mL | 2.6008 mL | |
| 30 mM | 0.0867 mL | 0.4335 mL | 0.8669 mL | 2.1674 mL | |
| 40 mM | 0.0650 mL | 0.3251 mL | 0.6502 mL | 1.6255 mL | |
| 50 mM | 0.0520 mL | 0.2601 mL | 0.5202 mL | 1.3004 mL | |
| 60 mM | 0.0433 mL | 0.2167 mL | 0.4335 mL | 1.0837 mL | |
| 80 mM | 0.0325 mL | 0.1626 mL | 0.3251 mL | 0.8128 mL |
Elafibranor Related Classifications
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