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Elafibranor (Alias: GFT505)

Name: Elafibranor
Brand: TargetMol
SKU: T4408
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

Catalog No. T4408 Copy Product Info

Purity: 98.78%

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Elafibranor (GFT505) is an agonist of the peroxisome proliferator-activated receptor-α (PPAR-α) and peroxisome proliferator-activated receptor-δ (PPAR-δ) with EC50 values of 45 and 175 nM, respectively.

Elafibranor

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Catalog No. T4408

Alias GFT505

Cas No. 923978-27-2

Pack Size	Price	USA Stock	Global Stock
2 mg	$30	In Stock	In Stock
5 mg	$48	In Stock	In Stock
10 mg	$64	In Stock	In Stock
25 mg	$112	In Stock	In Stock
50 mg	$186	In Stock	In Stock
100 mg	$297	In Stock	In Stock
200 mg	$449	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$52	In Stock	In Stock

In stock · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:98.78%

Appearance:Solid

Color:Yellow

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COA HPLC HNMR LCMS

Product Introduction

Bioactivity

Description	Elafibranor (GFT505) is an agonist of the peroxisome proliferator-activated receptor-α (PPAR-α) and peroxisome proliferator-activated receptor-δ (PPAR-δ) with EC50 values of 45 and 175 nM, respectively.
Targets&IC50	PPARα:45 nM (EC50), PPARδ:175 nM (EC50)
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.
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
Synonyms	GFT505

Chemical Properties

Molecular Weight	384.49
Formula	C₂₂H₂₄O₄S
Cas No.	923978-27-2
Smiles	CSc1ccc(cc1)C(=O)\C=C\c1cc(C)c(OC(C)(C)C(O)=O)c(C)c1
Relative Density.	1.21 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 125 mg/mL (325.11 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.2 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6008 mL	13.0042 mL	26.0085 mL	130.0424 mL
5 mM	0.5202 mL	2.6008 mL	5.2017 mL	26.0085 mL
10 mM	0.2601 mL	1.3004 mL	2.6008 mL	13.0042 mL
20 mM	0.1300 mL	0.6502 mL	1.3004 mL	6.5021 mL
50 mM	0.0520 mL	0.2601 mL	0.5202 mL	2.6008 mL
100 mM	0.0260 mL	0.1300 mL	0.2601 mL	1.3004 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc