Elafibranor

SKU: orb1223638

Description

A nove, potent dual PPAR α/δ agonist with EC50 of 45 and 175 nM, respectively; demonstrates liver-protective effects on steatosis, inflammation, and fibrosis in animal models of NAFLD/NASH and liver fibrosis; significantly reduces fasting plasma triglycerides and increases HDL cholesterol, also reduces γ glutamyl transferase levels.Diabetes Phase 3 Clinical(In Vitro):Elafibranor (GFT505) is being developed as a dual PPAR-α/PPAR-δ agonist for the treatment 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.(In Vivo):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 glucose homeostasis, and lipid metabolism and reduces inflammation. Elafibranor (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 Elafibranor. Elafibranor does not induce cardiac adverse effects of PPARγ-activating agonists in monkeys.

Key Properties

• CAS Number: 923978-27-2
• MW: 384.4886
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₄O₄S
• SMILES: CC(C)(OC1=C(C)C=C(/C=C/C(C2=CC=C(SC)C=C2)=O)C=C1C)C(O)=O
• Target: PPAR
• Solubility: DMSO: ≥ 33 mg/mL

Bioactivity

• In Vivo:
  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 glucose homeostasis, and lipid metabolism and reduces inflammation. Elafibranor (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 Elafibranor. Elafibranor does not induce cardiac adverse effects of PPARγ-activating agonists in monkeys.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GFT-505

Quick Database Links

Gene Symbol

PPAR