<Suppliers Price>

Elafibranor

Names

[ CAS No. ]:
923978-27-2

[ Name ]:
Elafibranor

[Synonym ]:
UNII-2J3H5C81A5
2-(2,6-Dimethyl-4-{(1E)-3-[4-(methylsulfanyl)phenyl]-3-oxo-1-propen-1-yl}phenoxy)-2-methylpropanoic acid
Propanoic acid, 2-[2,6-dimethyl-4-[(1E)-3-[4-(methylthio)phenyl]-3-oxo-1-propen-1-yl]phenoxy]-2-methyl-
GFT505
Elafibranor
2-[2,6-Dimethyl-4-[(1E)-3-[4-(methylthio)phenyl]-3-oxo-1-propen-1-yl]phenoxy]-2-methylpropanoic acid

Biological Activity

[Description]:

Elafibranor is a PPARα/δ agonist with EC50s of 45 and 175 nM, respectively.

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> PPAR
Research Areas >> Metabolic Disease

[Target]

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[1].

[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[1]. 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[2]. 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[3].

[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.

[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.

[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


[Related Small Molecules]

GW9662 | Retinoic acid | GW501516 | Troglitazone | T0070907 | Pemafibrate | CDDO-Im | Wy-14643 | GW0742 | GW1929 | FH535 | Icariin | Daidzein | Fisetin | GSK0660

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
569.0±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C22H24O4S

[ Molecular Weight ]:
384.489

[ Flash Point ]:
297.9±30.1 °C

[ Exact Mass ]:
384.139526

[ LogP ]:
5.63

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.606

[ Storage condition ]:
2-8°C

Related Compounds