| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. Cell Cytotoxicity Assay[2] Cell Line: | ||||||||||||
| 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]. Animal Model: | ||||||||||||
| Name | Aleglitazar | ||||||||||||
| CAS | 475479-34-6 | ||||||||||||
| Formula | C24H23NO5S | ||||||||||||
| Molar Mass | 437.51 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Bénardeau A, Benz J, Binggeli A, et al. Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes. Bioorg Med Chem Lett. 2009 May 1;19(9):2468-73. [2]. Yan Chen, et al. Aleglitazar, a dual peroxisome proliferator-activated receptor-α and -γ agonist, protects cardiomyocytes against the adverse effects of hyperglycaemia. Diab Vasc Dis Res. 2017 Mar; 14(2): 152–162. [3]. Valérie Boujon, et al. Dual PPARα/γ agonist aleglitazar confers stroke protection in a model of mild focal brain ischemia in mice. J Mol Med (Berl). 2019; 97(8): 1127-1138. |