Aleglitazaris a Potent Dual PPARα/γ Agonist

Aleglitazar (R1439) is a potent dual PPARα/γ agonist. And the IC50s are 38 nM and 19 nM for human PPARa and PPARγ, respectively.  Furthermore, Aleglitazar can be used for the research of type II diabetes.

In vitro, Aleglitazar exhibits species selectivity with respect to PPARα. Besides, the EC50s are 50 nM, 2.26 µM and 2.34 µM for human PPARα, rat PPARα, and mouse PPARα, respectively.

Besides, In human cardiomyocytes (HCM), wild-type mice cardiomyocytes (mCM-WT) cells. Aleglitazar does not significantly increase lactate dehydrogenase (LDH) release at 0.1-20 µM. However, there is a significant increase LDH release30-40 µM.
Aleglitazar dose-dependently decreases apoptosis. And, it also reduces caspase-3 activity and cytochrome-C release induced by HG.
And, this compound improves cell viability in cells exposed to hyperglycemia.

In vivo, Aleglitazar exerts beneficial effects on structural and functional outcomes of mild brain ischemia. What’s more, the dosages are 0.3 mg/kg and 3.0 mg/kg; intraperitoneal injection for 7 days.
As a result, Aleglitazar reduces key aspects of microglia activation. this includes NO production, release of pro-inflammatory cytokines, migration, and phagocytosis. And, as a model of middle cerebral artery occlusion (MCAO).

Aleglitazar attenuates inflammatory responses in the post-ischemic brain.
In conclusion, Aleglitazar is a new, potent, and balanced dual PPARalpha/gamma agonist. It has the potential for research of type II diabetes. A. Additionally, it also can be used for MCAO research.


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[2]. Yan Chen, et al. Diab Vasc Dis Res. 2017 Mar; 14(2): 152–162.