1. Cell Cycle/DNA Damage
  2. PPAR

Elafibranor (Synonyms: GFT505)

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

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

For research use only. We do not sell to patients.

Elafibranor Chemical Structure

Elafibranor Chemical Structure

CAS No. : 923978-27-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 840 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

View All PPAR Isoform Specific Products:

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target[1]

PPAR-α

45 nM (EC50)

PPAR-δ

175 nM (EC50)

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
Solvent & Solubility
In Vitro: 

DMSO : ≥ 33 mg/mL (85.83 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6008 mL 13.0042 mL 26.0085 mL
5 mM 0.5202 mL 2.6008 mL 5.2017 mL
10 mM 0.2601 mL 1.3004 mL 2.6008 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

384.49

Formula

C₂₂H₂₄O₄S

CAS No.

923978-27-2

SMILES

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

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

Purity: 99.31%

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Product Name:
Elafibranor
Cat. No.:
HY-16737
Quantity:

Elafibranor

Cat. No.: HY-16737