Edaglitazone

Names

[ Name ]:
Edaglitazone

[Synonym ]:
UNII:8GKF7V499B
EX-8519
5-({4-[2-(5-Methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]-1-benzothiophen-7-yl}methyl)-1,3-thiazolidine-2,4-dione
UNII-8GKF7V499B
Edaglitazone
2,4-Thiazolidinedione, 5-[[4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]benzo[b]thien-7-yl]methyl]-
5-((4-(2-(5-methyl-2-phenyloxazol-4-yl)ethoxy)benzo[b]thiophen-7-yl)methyl)thiazolidine-2,4-dione

Biological Activity

[Description]:

Edaglitazone is a potent, selective and orally active PPARγ agonist, with EC50s of 35.6 nM and 1053 nM for PPARα and PPARγ, respectively. Edaglitazone displays antiplatelet, antidiabetic and anti-hyperglycemic activity[1][2][3].

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> PPAR

[Target]

PPARγ:35.6 nM (EC50)

PPARα:1053 nM (EC50)

[In Vitro]

Edaglitazone (3-16 μM; 5 min) inhibits the collagen (1.2 μg/mL)-induced platelet aggregation. Edaglitazone increases the intraplatelet levels of cAMP in a concentration dependent manner. Edaglitazone preventes the Collagen-induced intraplatelet levels of PPARγ decrease[3].

[In Vivo]

Edaglitazone (4.4 mg/kg; p.o. daily for 10 days) enhances insulin sensitivity in obese rats[2].

[References]

[1]. Dietz M, et, al. Comparative molecular profiling of the PPARα/γ activator aleglitazar: PPAR selectivity, activity and interaction with cofactors. ChemMedChem. 2012 Jun;7(6):1101-11.

[2]. Fürnsinn C, et, al. Chronic and acute effects of thiazolidinediones BM13.1258 and BM15.2054 on rat skeletal muscle glucose metabolism. Br J Pharmacol. 1999 Nov;128(6):1141-8.

[3]. Muñoz-Gutiérrez C, et, al. Study of the interactions between Edaglitazone and Ciglitazone with PPARγ and their antiplatelet profile. Life Sci. 2017 Oct 1;186:59-65.