GFT-505; GFT505; Elafibranor; GFT 505
| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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Purity: =99.12%
Elafibranor (formerly GFT505) is a dual agonist of the PPARα/δ (peroxisome proliferator-activated receptor-α and -δ) with EC50 values of 45 and 175 nM, respectively. In addition to lowering inflammation, it can enhance insulin sensitivity, glucose homeostasis, and lipid metabolism. The treatment of T2DM, non-alcoholic fatty liver disease, insulin resistance, dyslipidemia, and other cardiometabolic disorders is currently being pursued with elafibranor. Both elafibranor and its active metabolite, GFT1007, exhibit strong agonist activity for PPAR-α and somewhat for PPAR-δ.
| Targets |
PPAR-α (IC50 = 45 nM); PPAR-δ (IC50 = 175 nM)
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|---|---|
| ln Vitro |
Elafibranor (GFT505) is being developed as a dual agonist for PPAR-α and PPAR-δ to inhibit non-alcoholic fatty liver disease and type 2 diabetes. GFT1007, an active metabolite of elafibranor, exhibits strong agonist activity for PPAR-α and somewhat for PPAR-δ[1].
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| ln Vivo |
Elafibranor is well tolerated; however, it does result in a slight, reversible elevation in serum creatinine and neither weight gain nor cardiac events. In addition to lowering inflammation, elafibranor enhances lipid metabolism and glucose homeostasis[2]. Treatment with elafibranor (GFT505) improves plasma lipids and glucose regulation in diabetic db/db mice. With Elafibranor, hepatic expression of the major gluconeogenic enzymes fructose 1,6-bisphosphatase 1 (FBP1), PEPCK, and glucose 6-phosphatase (G6Pase) is significantly dose-dependently reduced. In monkeys, PPARγ-activating agonists do not cause cardiac side effects when elabranor is used[3].
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| Enzyme Assay |
Elafibranor is an agonist of PPARα/δ with EC50 values of 45 and 175 nM, in that order. As a dual PPAR-α/PPAR-δ agonist, GFT505 is being developed to treat non-alcoholic fatty liver disease and type 2 diabetes. GThe active metabolite of GFT505, GFT1007, exhibits strong agonist activity for PPAR-α and to a lesser degree for PPAR-δ.
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| Cell Assay |
The drug was applied to the cells for a full day at the specified concentration.
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| Animal Protocol |
hApoE2 KI and hApoE2 KI/PPAR-α KO mice
30 mg/kg oral gavage |
| References |
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| Molecular Formula |
C22H24O4S
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| Molecular Weight |
384.49
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| Exact Mass |
384.14
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| Elemental Analysis |
C, 68.73; H, 6.29; O, 16.64; S, 8.34
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| CAS # |
923978-27-2
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| Related CAS # |
824932-88-9; 923978-27-2;
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| Appearance |
Solid powder
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| SMILES |
CC1=CC(=CC(=C1OC(C)(C)C(=O)O)C)/C=C/C(=O)C2=CC=C(C=C2)SC
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| InChi Key |
AFLFKFHDSCQHOL-IZZDOVSWSA-N
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| InChi Code |
InChI=1S/C22H24O4S/c1-14-12-16(13-15(2)20(14)26-22(3,4)21(24)25)6-11-19(23)17-7-9-18(27-5)10-8-17/h6-13H,1-5H3,(H,24,25)/b11-6+
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| Chemical Name |
2-[2,6-dimethyl-4-[(E)-3-(4-methylsulfanylphenyl)-3-oxoprop-1-enyl]phenoxy]-2-methylpropanoic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.87 mg/mL (7.46 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.17 mg/mL (5.64 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.17 mg/mL (5.64 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.17 mg/mL (5.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. Solubility in Formulation 5: ≥ 2.17 mg/mL (5.64 mM)(saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one),clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04526665 | Active Recruiting |
Drug: Elafibranor 80mg Drug: Placebo |
Primary Biliary Cirrhosis | Ipsen | September 24, 2020 | Phase 3 |
| NCT06016842 | Recruiting | Other: Matched 80 mg placebo Drug: Elafibranor |
Primary Biliary Cholangitis (PBC) |
Ipsen | August 31, 2023 | Phase 3 |
| NCT05627362 | Recruiting | Drug: Elafibranor 80 mg Drug: Elafibranor 120 mg |
Primary Sclerosing Cholangitis | Ipsen | January 27, 2023 | Phase 2 |
| NCT04171752 | Completed | Drug: elafibranor | Geriatrics Healthy |
Genfit | November 22, 2019 | Phase 1 |
| NCT05564208 | Completed | Drug: elafibranor | Healthy Participants | Ipsen | October 27, 2022 | Phase 1 |
Elafibranor-induced changes in glucose homeostasis markers in type 2 diabetic patients.Gastroenterology.2016 May;150(5):1147-1159.e5. |
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Changes from baseline in liver enzymes (A−C) and plasma lipids (D−F) in treatment groups of the Per Protocol set.
Overall improvement in liver histology in patients who achieved the primary outcome according to the modified definition of response in the elafibranor 120-mg arm. |
Changes from baseline in inflammatory markers (Sup2A) and in noninvasive scores of fibrosis and steatosis (Sup2B) in treatment groups in the per protocol analysis (n = 237).Gastroenterology.2016 May;150(5):1147-1159.e5. |
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