Elafibranor | CAS#923978-27-2 | PPA agonist

MedKoo Cat#: 561377 | Name: Elafibranor

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Elafibranor, also known as GFT-505, is a dual PPARα/δ agonist. is an agonist of the peroxisome proliferator-activated receptor-α and peroxisome proliferator-activated receptor-δ. GFT505 has an active metabolite, GFT1007, and both have potent agonist activity for PPAR-a and to a lesser extent for PPAR-d. Elafibranor improves insulin sensitivity, glucose homeostasis, and lipid metabolism and reduces inflammation. Elafibranor (GFT505) reverses nonalcoholic steatohepatitis (NASH) to prevent fibrosis progression. With an outstanding safety and tolerance profile, elafibranor provides NASH patients with needed cardio-protective benefits.

Chemical Structure

Elafibranor

CAS#923978-27-2

Theoretical Analysis

MedKoo Cat#: 561377

Name: Elafibranor

CAS#: 923978-27-2

Chemical Formula: C22H24O4S

Exact Mass: 384.1395

Molecular Weight: 384.49

Elemental Analysis: C, 68.73; H, 6.29; O, 16.64; S, 8.34

Price and Availability

Size	Price	Availability
10mg	USD 90.00	Ready to ship
25mg	USD 150.00	Ready to ship
50mg	USD 250.00	Ready to ship
100mg	USD 450.00	Ready to ship
200mg	USD 750.00	Ready to ship
500mg	USD 1,650.00	Ready to ship
1g	USD 2,950.00	Ready to ship
2g	USD 5,250.00	Ready to ship

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Related CAS #

824932-88-9 923978-27-2

Synonym

Elafibranor; GFT505; GFT-505; GFT 505; GFT1007 (metabolite); GFT1007; GFT1007;

IUPAC/Chemical Name

2-[2,6-Dimethyl-4-[(E)-3-(4-methylsulfanylphenyl)-3-oxoprop-1-enyl]phenoxy]-2-methylpropanoic acid

InChi Key

AFLFKFHDSCQHOL-IZZDOVSWSA-N

InChi Code

InChI=1S/C22H24O4S/c1-14-12-16(13-15(2)20(14)26-22(3,4)21(24)25)6-11-19(23)17-7-9-18(27-5)10-8-17/h6-13H,1-5H3,(H,24,25)/b11-6+

SMILES Code

CC(C)(OC1=C(C)C=C(/C=C/C(C2=CC=C(SC)C=C2)=O)C=C1C)C(O)=O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#C9R12B17

QC Data

View QC data: current batch, Lot#C9R12B17

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

Elafibranor (GFT505) is a PPARα/δ agonist with EC50s of 45 and 175 nM, respectively.

In vitro activity:

‘hSKP-HPC NASH’ cultures exposed to elafibranor (10 μM and 30 μM) for 24 h showed a dose-dependent decrease in neutral lipids (Fig. 3A and B) without causing cytotoxicity (no decline in ATP levels, data not shown). The decrease in neutral lipids was confirmed by flow-cytometric analysis whereby the histogram for lipid staining shifted from the control (blue) to the right, NASH condition (purple) and subsequently gradually shifted to the left (green and brown) when increasing concentrations of elafibranor were added (Fig. 3C). This anti-steatotic property of elafibranor was quantified by measuring the median fluorescence intensity of the cells that stained positive for the lipid dye (Fig. 3D). Reference: Pharmacol Res. 2019 Jun;144:377-389. https://pubmed.ncbi.nlm.nih.gov/31028903/

In vivo activity:

In contrast, treatment with elafibranor in free choice hamsters resulted in substantial improvement of liver lesions (see representative pictures in Fig. 4). These benefits were confirmed with NAFLD activity scoring indicating lower steatosis (Fig. 4A), inflammation (Fig. 4B), ballooning (Fig. 4C) and fibrosis (Fig. 4D) scores. To further characterize the anti-fibrotic effect of elafibranor, automated fibrosis quantification was performed. As shown in Fig. 5, elafibranor treatment resulted in substantially lower collagen liver content. Accordingly, elafibranor significantly reduced phenotypic (Fig. 5A) and bulk (Fig. 5B) collagen fibrosis scores (both P < 0.05 vs. vehicle), while morphometric (Fig. 5C) and texture (Fig. 5D) scores remained unaltered. Reference: Metabolism. 2021 Apr;117:154707. https://www.metabolismjournal.com/article/S0026-0495(21)00007-X/fulltext

	Solvent	mg/mL	mM
Solubility
	DMSO	54.5	141.75
	Ethanol	60.0	156.05

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 384.49 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Boeckmans J, Buyl K, Natale A, Vandenbempt V, Branson S, De Boe V, Rogiers V, De Kock J, Rodrigues RM, Vanhaecke T. Elafibranor restricts lipogenic and inflammatory responses in a human skin stem cell-derived model of NASH. Pharmacol Res. 2019 Jun;144:377-389. doi: 10.1016/j.phrs.2019.04.016. Epub 2019 Apr 24. PMID: 31028903. 2. Briand F, Maupoint J, Brousseau E, Breyner N, Bouchet M, Costard C, Leste-Lasserre T, Petitjean M, Chen L, Chabrat A, Richard V, Burcelin R, Dubroca C, Sulpice T. Elafibranor improves diet-induced nonalcoholic steatohepatitis associated with heart failure with preserved ejection fraction in Golden Syrian hamsters. Metabolism. 2021 Apr;117:154707. doi: 10.1016/j.metabol.2021.154707. Epub 2021 Jan 11. PMID: 33444606. 3. Liu L, Liu C, Zhao M, Zhang Q, Lu Y, Liu P, Yang H, Yang J, Chen X, Yao Y. The pharmacodynamic and differential gene expression analysis of PPAR α/δ agonist GFT505 in CDAHFD-induced NASH model. PLoS One. 2020 Dec 16;15(12):e0243911. doi: 10.1371/journal.pone.0243911. PMID: 33326461; PMCID: PMC7743980.

In vitro protocol:

In vivo protocol:

1. Briand F, Maupoint J, Brousseau E, Breyner N, Bouchet M, Costard C, Leste-Lasserre T, Petitjean M, Chen L, Chabrat A, Richard V, Burcelin R, Dubroca C, Sulpice T. Elafibranor improves diet-induced nonalcoholic steatohepatitis associated with heart failure with preserved ejection fraction in Golden Syrian hamsters. Metabolism. 2021 Apr;117:154707. doi: 10.1016/j.metabol.2021.154707. Epub 2021 Jan 11. PMID: 33444606. 2. Liu L, Liu C, Zhao M, Zhang Q, Lu Y, Liu P, Yang H, Yang J, Chen X, Yao Y. The pharmacodynamic and differential gene expression analysis of PPAR α/δ agonist GFT505 in CDAHFD-induced NASH model. PLoS One. 2020 Dec 16;15(12):e0243911. doi: 10.1371/journal.pone.0243911. PMID: 33326461; PMCID: PMC7743980.

1: Khan AA, Ul Haq F, Wahab QMF, Aslam T, Khalid A, Ali A. Breaking Grounds: A Comprehensive Analysis of Cutting-Edge Treatments for Primary Biliary Cirrhosis/Primary Biliary Cholangitis With Futuristic Treatments. Cureus. 2025 Feb 24;17(2):e79582. doi: 10.7759/cureus.79582. PMID: 40151700; PMCID: PMC11946705. 2: Gul MH, Waheed A, Wardak AB, Shah Y, Azam Raja HA, Ilmaguook B, Hussaini H, Zafar F. Elafibranor: a breakthrough therapy revolutionizing primary biliary cholangitis (PBC) treatment. Ann Med Surg (Lond). 2025 Jan 31;87(2):454-456. doi: 10.1097/MS9.0000000000002794. PMID: 40110265; PMCID: PMC11918746. 3: Salamat Ali J, Salamat Ali T, Al Hasibuzzaman M. Latest FDA approved drug Elafibranor (Iqirvo): a novel prospect for treatment of primary biliary cholangitis. Ann Med Surg (Lond). 2025 Jan 9;87(1):30-32. doi: 10.1097/MS9.0000000000002868. PMID: 40109633; PMCID: PMC11918794. 4: Farhadi S, Mohammadi S, AlKindi AY, Al-Amri IS. Therapeutic potential of elafibranor in alcohol-associated liver disease: Insights into macrophage modulation and fibrosis reduction. World J Biol Chem. 2025 Mar 5;16(1):104535. doi: 10.4331/wjbc.v16.i1.104535. PMID: 40070853; PMCID: PMC11891553. 5: One-Year Treatment With Elafibranor in the Phase 3 ELATIVE Trial Improves GLOBE and UK-PBC Prognostic Scores. Gastroenterol Hepatol (N Y). 2024 Dec;20(12 Suppl 12):9-10. PMID: 39897515; PMCID: PMC11784548. 6: Elafibranor Long-Term Efficacy and Safety and Impact on Fatigue in Primary Biliary Cholangitis: Interim Results From the Open-Label Extension of the ELATIVE Trial Up to 3 Years. Gastroenterol Hepatol (N Y). 2024 Dec;20(12 Suppl 12):3-4. PMID: 39897512; PMCID: PMC11784550. 7: Pirola L. Elafibranor, a dual PPARα and PPARδ agonist, reduces alcohol- associated liver disease: Lessons from a mouse model. World J Gastroenterol. 2025 Jan 28;31(4):99312. doi: 10.3748/wjg.v31.i4.99312. PMID: 39877705; PMCID: PMC11718637. 8: Cheng CH, Hao WR, Cheng TH. Elafibranor: A promising therapeutic approach for liver fibrosis and gut barrier dysfunction in alcohol-associated liver disease. World J Gastroenterol. 2025 Jan 21;31(3):98783. doi: 10.3748/wjg.v31.i3.98783. PMID: 39839906; PMCID: PMC11684164. 9: Seladelpar (Livdelzi) for primary biliary cholangitis. Med Lett Drugs Ther. 2025 Jan 20;67(1720):13-15. doi: 10.58347/tml.2025.1720d. PMID: 39819989. 10: Cui WT, Xue HR, Wei DF, Feng XY, Wang K. Prospects of elafibranor in treating alcohol-associated liver diseases. World J Gastroenterol. 2025 Jan 14;31(2):99549. doi: 10.3748/wjg.v31.i2.99549. PMID: 39811505; PMCID: PMC11684193. 11: Lee D, Jung K, Lee J, Kang HJ, Lee JY, Kim J, Ham D, Cho J, Eom DW, Kang KS. Role of 11β-hydroxysteroid dehydrogenase type 1 inhibition in the antiobesity effect of J2H-1702 on adipocytes and a high-fat diet-induced NASH model. Eur J Pharmacol. 2025 Feb 15;989:177272. doi: 10.1016/j.ejphar.2025.177272. Epub 2025 Jan 12. PMID: 39809350. 12: Madariaga Traconis AP, Uribe-Esquivel M, Barbero Becerra VJ. Exploring the Role of Peroxisome Proliferator-Activated Receptors and Endothelial Dysfunction in Metabolic Dysfunction-Associated Steatotic Liver Disease. Cells. 2024 Dec 12;13(24):2055. doi: 10.3390/cells13242055. PMID: 39768147; PMCID: PMC11674254. 13: Elafibranor (Iqirvo) for primary biliary cholangitis. Med Lett Drugs Ther. 2024 Dec 23;66(1718):202-204. doi: 10.58347/tml.2024.1718b. PMID: 39762188. 14: Warsop Z, Anand N, Al Maliki H, De Souza S, Kamyab A, Al Hadad A, Alrubaiy L. Up-to-Date Snapshot of Current and Emerging Medical Therapies in Primary Biliary Cholangitis. J Pers Med. 2024 Nov 30;14(12):1133. doi: 10.3390/jpm14121133. PMID: 39728045; PMCID: PMC11678846. 15: Giannini EG, Pasta A, Calabrese F, Labanca S, Marenco S, Pieri G, Plaz Torres MC, Strazzabosco M. Second-Line Treatment for Patients With Primary Biliary Cholangitis: A Systematic Review With Network Meta-Analysis. Liver Int. 2025 Jan;45(1):e16222. doi: 10.1111/liv.16222. PMID: 39720853; PMCID: PMC11669080. 16: Levy C, Bowlus CL. Primary biliary cholangitis: Personalizing second-line therapies. Hepatology. 2024 Nov 12. doi: 10.1097/HEP.0000000000001166. Epub ahead of print. PMID: 39707635. 17: Hayes CM, Gallucci GM, Boyer JL, Assis DN, Ghonem NS. PPAR agonists for the treatment of cholestatic liver diseases: Over a decade of clinical progress. Hepatol Commun. 2024 Dec 20;9(1):e0612. doi: 10.1097/HC9.0000000000000612. PMID: 39699308; PMCID: PMC11661771. 18: Ahmed IF, Rizwan F, Mansoor H, Fakhoury M, Shaik MH, Gandhi F, Belletieri C. Elafibranor (Iqirvo) unveiled: a groundbreaking FDA-approved therapy revolutionizing primary biliary cholangitis treatment. Ann Med Surg (Lond). 2024 Oct 17;86(12):6910-6912. doi: 10.1097/MS9.0000000000002672. PMID: 39649939; PMCID: PMC11623839. 19: Cumpian NA, Choi G, Saab S. Review of Current and Upcoming Second-Line Treatments for Primary Biliary Cholangitis. Dig Dis Sci. 2025 Jan;70(1):100-110. doi: 10.1007/s10620-024-08742-w. Epub 2024 Dec 2. PMID: 39621183. 20: Sun YQ, Wu Y, Li MR, Wei YY, Guo M, Zhang ZL. Elafibranor alleviates alcohol-related liver fibrosis by restoring intestinal barrier function. World J Gastroenterol. 2024 Nov 21;30(43):4660-4668. doi: 10.3748/wjg.v30.i43.4660. PMID: 39575408; PMCID: PMC11572637.