1. Cell Cycle/DNA Damage
    NF-κB
  2. PPAR

Elafibranor (Synonyms: GFT505)

Cat. No.: HY-16737 Purity: 99.31%
Data Sheet SDS Handling Instructions

Elafibranor is an agonist of the peroxisome proliferator-activated receptor-α (PPAR-α) and peroxisome proliferator-activated receptor-δ (PPAR-δ) with EC50 values of 45 and 175 nM, respectively.

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Elafibranor Chemical Structure

Elafibranor Chemical Structure

CAS No. : 923978-27-2

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10 mM * 1 mL in DMSO $66 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Elafibranor is an agonist of the peroxisome proliferator-activated receptor-α (PPAR-α) and peroxisome proliferator-activated receptor-δ (PPAR-δ) with EC50 values of 45 and 175 nM, respectively.

IC50 & Target

EC50: 45 nM (PPAR-α), 175 nM (PPAR-δ)[1]

In Vitro

GFT505 is being developed as a dual PPAR-α/PPAR-δ agonist for the treatment of T2DM and non-alcoholic fatty liver disease. GFT505 has an active metabolite, GFT1007, and both have potent agonist activity for PPAR-α and to a lesser extent for PPAR-δ[1].

In Vivo

GFT505 improves insulin sensitivity and early studies indicate it may be useful in non-alcoholic fatty liver disease which is being tested in a Phase IIb study[1]. Elafibranor is well tolerated and does not cause weight gain or cardiac events, but does produce a mild, reversible increase in serum creatinine. Elafibranor improves insulin sensitivity, glucose homeostasis, and lipid metabolism and reduces inflammation[2]. GFT505 treatment improves glucose control and plasma lipids in diabetic db/db mice. A significant dose-dependent reduction of hepatic expression of the key gluconeogenic enzymes glucose 6-phosphatase (G6Pase), PEPCK, and fructose 1,6-bisphosphatase 1 (FBP1) is observed with GFT505. GFT505 does not induce cardiac adverse effects of PPARγ-activating agonists in monkeys[3].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02704403 Genfit Nonalcoholic Steatohepatitis (NASH) With Fibrosis March 2016 Phase 3
NCT03124108 Genfit Primary Biliary Cholangitis (PBC) April 5, 2017 Phase 2
NCT02142127 Genfit|SGS Life Sciences Healthy April 2014 Phase 1
NCT01261494 Genfit Type II Diabetes Mellitus December 2010 Phase 2
NCT01271751 Genfit Atherogenic Dyslipidaemia|Abdominal Obesity January 2009 Phase 2
NCT01275469 Genfit Impaired Glucose Tolerance|Abdominal Obesity June 2009 Phase 2
NCT01271777 Genfit Insulin Resistance|Abdominal Obesity January 2011 Phase 2
NCT01694849 Genfit|Naturalpha|Premier Research Group plc Non-Alcoholic Steatohepatitis (NASH) September 2012 Phase 2
NCT02091310 Genfit|Eurofins Optimed|CardiaBase|PHINC DEVELOPMENT Healthy Volunteers February 2014 Phase 1
NCT01474161 Genfit|SGS Aster S.A.S.|Naturalpha Type 2 Diabetes|Diabetes Mellitus, Type 2|Metabolic Diseases|Cardiovascular Diseases|Obese|Dyslipidemia November 2011 Phase 1
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References
Molecular Weight

384.49

Formula

C₂₂H₂₄O₄S

CAS No.

923978-27-2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 33 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Elafibranor
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