Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | In stock | $ 59.00 | |
10 mg | In stock | $ 86.00 | |
25 mg | In stock | $ 137.00 | |
50 mg | In stock | $ 227.00 | |
100 mg | In stock | $ 398.00 | |
500 mg | In stock | $ 947.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 52.00 |
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 | PPAR-α:45 nM (EC50), PPAR-δ:175 nM (EC50) |
In vitro | GFT505 is being developed as a dual PPAR-α/PPAR-δ agonist for the treatment of T2DM and non-alcoholic fatty liver disease. GFT505 has an active metabolite, GFT1007, and both have potent agonist activity for PPAR-α and to a lesser extent for 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 |
Molecular Weight | 384.49 |
Formula | C22H24O4S |
CAS No. | 923978-27-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (130.04 mM)
You can also refer to dose conversion for different animals. More
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Elafibranor 923978-27-2 DNA Damage/DNA Repair Metabolism PPAR inhibit GFT-505 Peroxisome proliferator-activated receptors GFT 505 GFT505 Inhibitor inhibitor