Aleglitazar (R1439;RO0728804) 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 IC 50 s of 38 nM and 19 nM for human PPARa and PPARγ, respectively. Aleglitazar can be used for the research of type II diabetes.

Solid

PPARγ 19 nM (IC50) PPARα 38 nM (IC50

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.
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.
Aleglitazar (0.01-20?μM; 48?hours) decreases hyperglycaemic conditions (HG, glucose 25?mM)-induced apoptosis, caspase-3 activity and cytochrome-C release.
Aleglitazar improves cell viability in cells exposed to hyperglycaemia.
has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Aleglitazar reduces key aspects of microglia activation including NO production, release of proinflammatory cytokines, migration, and phagocytosis.
Aleglitazar attenuates inflammatory responses in post-ischemic brain.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : ≥ 50 mg/mL (114.28 mM)配制储备液