1. Cell Cycle/DNA Damage
  2. PPAR
  3. Elafibranor

Elafibranor (Synonyms: GFT505)

Cat. No.: HY-16737 Purity: 99.18%
Handling Instructions

Elafibranor (GFT505) 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

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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
25 mg USD 285 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 4 publication(s) in Google Scholar

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Description

Elafibranor (GFT505) 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

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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[2]. 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[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 33 mg/mL (85.83 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" 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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.17 mg/mL (5.64 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (5.64 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.18%

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Keywords:

ElafibranorGFT505GFT 505GFT-505PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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