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Elafibranor | PPARalpha/delta agonist

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

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Catalog#  10-3901-0005

$65.00
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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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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° (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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