Elafibranor | PPARalpha/delta agonist

CAS:
923978-27-2
Catalog Number:
10-3901
Activity:
PPARalpha/delta agonist
Chemical Name:
2-[2,6-Dimethyl-4-[(E)-3-(4-methylsulfanylphenyl)-3-oxoprop-1-enyl]phenoxy]-2-methylpropanoic acid
Alternate Name:
GFT505
Molecular Weight:
384.49
Molecular Formula:
C22H24O4S
Solubility:
Soluble in DMSO (up to at least 25 mg/ml).
Physical Properties:
Pale yellow solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$65.00
25 mg$235.00

Elafibranor (923978-27-2) is a dual PPARα/δ agonist (EC50 PPARα = 10-20 nM; PPARδ = 100-150 nM).1 It was able to decrease plasma triglycerides levels1, increase HDL cholesterol levels in human studies1, and improve hepatic and peripheral insulin sensitivity2. Elafibranor’s antidiabetic effects in db/db were without the adverse cardiac effects seen in PPARγ agonism.3 Elafibranor has also been shown to have therapeutic promise in the treatment of nonalcoholic steatohepatitis (NASH).4-6

References/Citations:

1) Cariou et al. (2011) Effects of the New Dual PPARα/δ Agonist GFT505 on Lipid and Glucose Homeostasis in Abdominally Obese Patients With Combined Dyslipidemia or Impaired Glucose Metabolism; Diabetes Care 34 2008
2) Cariou et al. (2013) Dual peroxisome proliferator receptor α/δ agonist GFT505 improves hepatic and peripheral insulin sensitivity in abdominally obese subjects; Diabetes Care 36 2923
3) Hanf et al. (2014) The dual peroxisome proliferator-activated 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. 11 440
4) Staels et al. (2013) Hepatoprotective effects of the dual peroxisome proliferator-activated receptor alpha-delta agonist, GFT505, in rodent models of nonalcoholic fatty liver disease/nonalcoholic steatohepatitis; Hepatology 58 1941
5) Ratziu et al. (2016) Elafibranor, an Agonist of the Peroxisome Proliferator-Activated Receptor-α and -δ, Induces Resolution of Nonalcoholic Steatohepatitis Without Fibrosis Worsening.; Gastroenterology. 39 2951
6) Boeckmans et al. (2019) Elafibranor restricts lipogenic and inflammatory responses in a human skin stem cell-derived model of NASH.; Pharmacol. Res. 114 377

CAS:
923978-27-2
Catalog Number:
10-3901
Activity:
PPARalpha/delta agonist
Chemical Name:
2-[2,6-Dimethyl-4-[(E)-3-(4-methylsulfanylphenyl)-3-oxoprop-1-enyl]phenoxy]-2-methylpropanoic acid
Alternate Name:
GFT505
Molecular Weight:
384.49
Molecular Formula:
C22H24O4S
Solubility:
Soluble in DMSO (up to at least 25 mg/ml).
Physical Properties:
Pale yellow solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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