Elafibranor

SKU: orb1302884

Description

Elafibranor

Research Area

Metabolism Research, Molecular Biology

Key Properties

• CAS Number: 923978-27-2
• MW: 384.5
• Purity: >98%
• Formula: C₂₂H₂₄O₄S
• SMILES: CSc1ccc(cc1)C(=O)\C=C\c1cc(C)c(OC(C)(C)C(O)=O)c(C)c1
• Target: Transcription factor
• Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Bioactivity

• Target IC50:
  PPARδ:175 nM (EC50)|PPARα:45 nM (EC50)
• 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. 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. 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
• In Vitro:
  GFT505, under development as a dual PPAR-α/δ agonist, targets both Type 2 Diabetes Mellitus (T2DM) and non-alcoholic fatty liver disease. It, alongside its active metabolite GFT1007, exhibits strong agonistic activity for PPAR-α and, to a lesser extent, PPAR-δ.

Storage & Handling

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

Alternative Names

GFT505

Compound Identifiers

PubChem CID

9864881