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  3. Elafibranor

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
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10 mM * 1 mL in DMSO USD 66 In-stock
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5 mg USD 79 In-stock
10 mg USD 132 In-stock
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50 mg USD 420 In-stock
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Based on 10 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 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[1].

MedChemExpress (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].

MedChemExpress (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.
Appearance

Solid

Color

Light yellow to yellow

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 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : ≥ 33 mg/mL (85.83 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: 2.87 mg/mL (7.46 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    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

    This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.13%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6008 mL 13.0042 mL 26.0085 mL 65.0212 mL
5 mM 0.5202 mL 2.6008 mL 5.2017 mL 13.0042 mL
10 mM 0.2601 mL 1.3004 mL 2.6008 mL 6.5021 mL
15 mM 0.1734 mL 0.8669 mL 1.7339 mL 4.3347 mL
20 mM 0.1300 mL 0.6502 mL 1.3004 mL 3.2511 mL
25 mM 0.1040 mL 0.5202 mL 1.0403 mL 2.6008 mL
30 mM 0.0867 mL 0.4335 mL 0.8669 mL 2.1674 mL
40 mM 0.0650 mL 0.3251 mL 0.6502 mL 1.6255 mL
50 mM 0.0520 mL 0.2601 mL 0.5202 mL 1.3004 mL
60 mM 0.0433 mL 0.2167 mL 0.4335 mL 1.0837 mL
80 mM 0.0325 mL 0.1626 mL 0.3251 mL 0.8128 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Elafibranor
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