| 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. |
| Solubility Information | DMSO : 50 mg/mL (130.04 mM)
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| Keywords | inhibit | GFT-505 | PPAR | Peroxisome proliferator-activated receptors | GFT 505 | Elafibranor | Inhibitor |
| Inhibitors Related | PHYTOL | (S)-(+)-Ibuprofen | BADGE | Cinnamyl alcohol | Daidzein | Fenofibrate | Pioglitazone hydrochloride | 5-Aminosalicylic Acid | Naringenin | Fisetin | 2,3-Butanediol | Icariin |
| Related Compound Libraries | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Anti-Diabetic Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Drug Library |
United States
