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Chemical Structure| 923978-27-2 Chemical Structure| 923978-27-2

Structure of Elafibranor
CAS No.: 923978-27-2

Chemical Structure| 923978-27-2

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Elafibranor is an agonist of PPARα and PPARδ with EC50 values of 45 nM and 175 nM, respectively. Elafibranor also attenuates nonalcoholic steatohepatitis without fibrosis worsening.

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Product Details of Elafibranor

CAS No. :923978-27-2
Formula : C22H24O4S
M.W : 384.49
SMILES Code : CC(C)(OC1=C(C)C=C(/C=C/C(C2=CC=C(SC)C=C2)=O)C=C1C)C(O)=O
MDL No. :MFCD27987940
InChI Key :AFLFKFHDSCQHOL-IZZDOVSWSA-N
Pubchem ID :9864881

Safety of Elafibranor

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HepG2/LX-2 (24:1 ratio) 50 μM 48 hours Elafibranor prevented fat accumulation and reduced COL1A1 levels Int J Mol Sci. 2019 Apr 2;20(7):1629
LX-2 cells 0-30 μM 24-48 hours EFN had no direct effect on cell proliferation or profibrogenic activity in EtOH-stimulated LX-2 cells. World J Gastroenterol. 2024 Jul 28;30(28):3428-3446
Caco-2 cells 0-30 μM 120 minutes to 48 hours EFN restored tight junction protein expression and improved intestinal barrier function by PPARδ activation, reducing EtOH-induced permeability and apoptosis in Caco-2 cells. World J Gastroenterol. 2024 Jul 28;30(28):3428-3446
HepG2 cells 0-30 μM 24-48 hours EFN promoted lipolysis and β-oxidation and enhanced autophagic and antioxidant capacities in EtOH-stimulated HepG2 cells, primarily through PPAR α activation. World J Gastroenterol. 2024 Jul 28;30(28):3428-3446

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice HuMgat2 mouse model Oral 30 mg/kg Continued for 16 weeks To evaluate the therapeutic effects of Elafibranor on MASH phenotypes, results showed that Elafibranor attenuated multiple MASH-related phenotypes, including fat deposition, fibrosis, and inflammatory responses. J Lipid Res. 2024 Dec;65(12):100695
C57BL/6J mice Alcohol-associated liver disease model Oral gavage 3 and 10 mg/kg/day Daily administration for 8 weeks EFN attenuated ALD-related liver fibrosis by inhibiting lipid accumulation and apoptosis, enhancing hepatocyte autophagic and antioxidant capacities, and suppressing LPS/TLR4/NF-κB-mediated inflammatory responses through restoration of intestinal barrier function. World J Gastroenterol. 2024 Jul 28;30(28):3428-3446

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03844555 Renal Impairment|Renal Insuffi... More >>ciency|Kidney Diseases|Pharmacokinetics Less << PHASE1 COMPLETED 2020-03-21 Eurofins Optimed, Gières, 3861... More >>0, France|ARENSIA Exploratory Medicine Unit, Nephrology Hospital Dr. Carol Davilla, Bucharest, 010701, Romania Less <<
NCT05543369 Healthy Volunteers PHASE1 COMPLETED 2023-03-10 Collaborative Neuroscience Res... More >>earch LLC, Long Beach, California, 90806, United States|Collaborative Neuroscience Research, LLC, Los Alamitos, California, 90720, United States Less <<
NCT06730061 Primary Biliary Cholangitis PHASE3 RECRUITING 2032-04-08 Nippon Medical School - Chiba ... More >>Hokusoh Hospital, Chiba, Japan|Fukushima Medical University Hospital, Fukushima, Japan|Chugoku Rosai Hospital, Hiroshima, Japan|Teine Keijinkai Hospital, Hokkaido, Japan|Kagawa University Hospital, Kagawa, Japan|Kagoshima University Hospital, Kagoshima, Japan|Shinshu University Hospital, Nagano, Japan|National Hospital Organization Nagasaki Medical Center, Nagasaki, Japan|Nara Medical University Hospital, Nara, Japan|Nagaoka Red Cross Hospital, Niigata, Japan|Niigata University Medical & Dental Hospital, Niigata, Japan|National Hospital Organization Osaka National Hospital, Osaka, Japan|Hamamatsu University Hospital, Shizuoka, Japan|Juntendo University Hospital, Tokyo, Japan|Teikyo University Hospital, Tokyo, Japan|Tokyo Metropolitan Komagome Hospital, Tokyo, Japan Less <<
NCT03765671 Hepatic Impairment|Liver Disea... More >>se|Pharmacokinetics Less << PHASE1 COMPLETED 2019-06-14 Division of Clinical Pharmacol... More >>ogy, University of Miami, Miami, Florida, 33136, United States|inVentiv Health Clinical Research, Miami, Florida, 33136, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.60mL

0.52mL

0.26mL

13.00mL

2.60mL

1.30mL

26.01mL

5.20mL

2.60mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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