Tesaglitazar

Peroxisome proliferator-activated receptors (PPARs) are activated by fatty acids and eicosanoids as well as antidyslipidemic agents. Among the receptor isotypes, PPARα demonstrates a particular role in fatty acid oxidation whereas PPARγ is known to be involved in adipocyte differentiation and lipid storage. Tesaglitazar, a dihydro cinnamate derivative, is a dual agonist of PPARα and γ that demonstrates IC₅₀ values of 1 and 0.2 µM, respectively in ligand binding assays.¹ At 3 µM/kg/day for three weeks, tesaglitazar has been used to reduce insulin resistance in obese Zucker rats.² Furthermore, it has been investigated clinically for its potential to address disorders in glucose and lipid metabolism in patients with type 2 diabetes.³

WARNING This product is not for human or veterinary use.

1. Cronet, P., Petersen, J.F.W., Folmer, R., et al. Structure of the PPARα and -γ ligand binding domain in complex with AZ 242; ligand selectivity and agonist activation in the PPAR family. Structure 9(8), 699-706 (2001).

2. Wallenius, K., Kjellstedt, A., Thalén, P., et al. The PPARα/γ agonist, tesaglitazar, improves insulin mediated switching of tissue glucose and free fatty acid utilization in vivo in the obese Zucker rat. PPAR Res. 305347 (2013).

3. Wilding, J.P.H., Gause-Nilsson, I., Persson, A., et al. Tesaglitazar, as add-on therapy to sulphonylurea, dose-dependently improves glucose and lipid abnormalities in patients with type 2 diabetes. Diab. Vasc. Dis. Res. 4(3), 194-203 (2007).