Aleglitazar

Aleglitazar (R1439) is a potent dual PPARα/γ agonist, with IC₅₀s of 38 nM and 19 nM for human PPARa and PPARγ, respectively. Aleglitazar can be used for the research of type II diabetes^[1]. In Vitro: Aleglitazar exhibits species selectivity with respect to PPARα, with an EC₅₀s of 50 nM, 2.26 µM and 2.34 µM for human PPARα, rat PPARα and mouse PPARα, respectively^[1].
Aleglitazar (0.01-40 µM; 12-48 hours) does not significantly increase lactate dehydrogenase (LDH) release at concentrations of 0.1 µM to 20 µM, but significant increases LDH release at concentrations of 30 µM and 40 µM^[2].
Aleglitazar (0.01-20 µM; 48 hours) decreases hyperglycaemic conditions (HG, glucose 25 mM)-induced apoptosis, caspase-3 activity and cytochrome-C release^[2].
Aleglitazar improves cell viability in cells exposed to hyperglycaemia^[2].
In Vivo: Aleglitazar (0.3-3.0 mg/kg; i.p.; daily; for 7 days) exerts beneficial effects on structural and functional outcomes of mild brain ischemia^[3].
Aleglitazar reduces key aspects of microglia activation including NO production, release of proinflammatory cytokines, migration, and phagocytosis^[3].
Aleglitazar attenuates inflammatory responses in post-ischemic brain^[3].