Elafibranor (Synonyms: GFT505)

Name: Elafibranor
Brand: MedChemExpress
SKU: HY-16737
Rating: 5.0 (16 reviews)

Cat. No.: HY-16737 Purity: 99.66%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Elafibranor (GFT505) is a PPARα/δ agonist with EC₅₀s of 45 and 175 nM, respectively. Elafibranor can be used for the study of primary biliary cholangitis.

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

CAS No. : 923978-27-2

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of Elafibranor:

(E/Z)-Elafibranor In-stock
Elafibranor (Standard) Get quote

16 Publications Citing Use of MCE Elafibranor

Cell Imaging/Staining

Bio/Physico-chemical Assay

: Elafibranor purchased from MedChemExpress. Usage Cited in: Biomaterials. 2022 Nov:290:121817. [Abstract]; Elafibranor (30 μM; 10 d) prevented FFA-induced lipid uptake of NAFLD MCLS.

: Elafibranor purchased from MedChemExpress. Usage Cited in: Biomaterials. 2022 Nov:290:121817. [Abstract]; Elafibranor (30 μM; 48 h) significantly reduced the protein expression levels of Collagen 1 of NAFLD MCLS in the NASH conditions.

: Elafibranor purchased from MedChemExpress. Usage Cited in: Biomaterials. 2021 Sep:276:121006.; Elafibranor (ELN) (30 μM; 3 d) reduced BODIPY® staining in hEPSC HepMat co-cultures co-treated with OA.

: Elafibranor purchased from MedChemExpress. Usage Cited in: Biomaterials. 2021 Sep:276:121006.; Relative expression of fibrogenic and proinflammatory marker genes, and secreted pro-collagen, TNF-α, IL1α, and IL6 in d32 hESC-derived HepMat co-cultures was assessed. Elafibranor (ELN) (30 μM; 3–7 d) decreased COL1A1, COL3A1, and COL5A2 levels in hEPSC HepMat co-cultures.

: Elafibranor purchased from MedChemExpress. Usage Cited in: Acta Biomater. 2021 Oct 15:134:228-239. [Abstract]; Elafibranor (ELA) (10-30 μM) could prevent the formation of lipid droplets in on-chip NAFLD.

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PPARα PPARβ/δ PPARγ PPAR PPARδ

Biological Activity
Purity & Documentation
References
Customer Review

Description

Elafibranor (GFT505) is a PPARα/δ agonist with EC₅₀s of 45 and 175 nM, respectively. Elafibranor can be used for the study of primary biliary cholangitis^[1].

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.

923978-27-2

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
10 mM	0.2601 mL	1.3004 mL	2.6008 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 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.17 mg/mL (5.64 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.17 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 99.66%

Select Batch:

Data Sheet (273 KB) SDS (393 KB)

COA (244 KB) HNMR (146 KB) LCMS (99 KB)

Handling Instructions (2659 KB)

References

[1]. Liu ZM, et al. Early investigational drugs targeting PPAR-α for the treatment of metabolic disease.Expert Opin Investig Drugs. 2015 May;24(5):611-21. [Content Brief]

[2]. Ratziu V, et al. Elafibranor, an Agonist of the Peroxisome Proliferator-Activated Receptor-α and -δ, Induces Resolution of Nonalcoholic Steatohepatitis Without Fibrosis Worsening. Gastroenterology. 2016 May;150(5):1147-1159. [Content Brief]

[3]. Hanf R, et al. The dual peroxisome proliferator-activated receptor alpha/delta agonist GFT505 exerts anti-diabetic effects in db/db mice without peroxisome proliferator-activated receptor gamma-associated adverse cardiac effects.Diab Vasc Dis Res. 2014 No [Content Brief]

Complete Stock Solution Preparation Table

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

Elafibranor Related Classifications

Metabolic Disease Inflammation/Immunology

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.

Keywords:

Elafibranor923978-27-2GFT505GFT 505GFT-505PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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Elafibranor (Synonyms: GFT505)

Customer Review

Other Forms of Elafibranor:

Elafibranor Related Antibodies

16 Publications Citing Use of MCE Elafibranor

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PPAR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Elafibranor Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Elafibranor Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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