| Name | Elafibranor |
| 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. |
| 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 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.2 mM), Sonication is recommended.
DMSO : 125 mg/mL (325.11 mM), Sonication is recommended.
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| Keywords | PPARδ | PPARα | PPAR | Peroxisome proliferator-activated receptors | Inhibitor | inhibit | GFT-505 | GFT 505 | Elafibranor |
| Inhibitors Related | PHYTOL | Rosiglitazone | Retinoic acid | Daidzein | Fenofibrate | Magnesium acetate tetrahydrate | Maltitol | Naringenin | 2,3-Butanediol | NPC 15199 | Icariin | Cloxiquine |
| Related Compound Libraries | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Stem Cell Differentiation Compound Library | Mitochondria-Targeted Compound Library | FDA-Approved Drug Library | Anti-Cancer Approved Drug Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
