Aleglitazar 是一种高效的 PPARα/γ 双重激动剂，对人 PPARα 和 PPARγ 作用的 IC50 分别为 38 nM 和 19 nM。Aleglitazar 可用于 II 型糖尿病的研究。

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.

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].

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].

475479-34-6

C24H23NO5S

437.51

RO0728804;R1439

DMSO:45mg/mL (102.9mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years