PPARα/γ agonist 2

Names

[ CAS No. ]:
2213365-56-9

[ Name ]:
PPARα/γ agonist 2

Biological Activity

[Description]:

PPARα/γ agonist 2 is an orally active PPARα full agonist and PPARγ partial agonist. PPARα/γ agonist 2 activates PPARα and PPARγ with EC50 values of 0.95 μM and 0.91 μM respectively. PPARα/γ agonist 2 is also a PTP1B inhibitor. PPARα/γ agonist 2 is an anti-diabetic agent[1].

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> PPAR
Research Areas >> Metabolic Disease

[Target]

PPARα:0.95 μM (EC50)

PPARγ:0.91 μM (EC50)


[In Vitro]

PPARα/γ agonist 2 (化合物 10) 有效抑制 PTP1B，IC50 为 13.2 μM (动力学测定)[1]。 PPARα/γ agonist 2 (25 μM，30 分钟) 在 C2C12 细胞中以胰岛素-非依赖性机制增强葡萄糖的摄取，并且比 UK5099 (HY-15475) 更有效[1]。 PPARα/γ agonist 2 (25 μM，30 分钟) 降低 C2C12 细胞中的线粒体膜电位[1]。

[In Vivo]

PPARα/γ agonist 2 (化合物 10) (25 and 50 mg/kg, p.o.) 降低 STZ 诱导的糖尿病小鼠的血糖水平和脂质含量[1]。 Animal Model: STZ-induced diabetic mice[1] Dosage: 25 and 50 mg/kg Administration: p.o. Result: Reduced the levels of TC, HDL, LDL-C, VLDL-C, and TG. Brought diabetes-induced hyperlipidemia back to normal.

[References]

[1]. Laghezza A, et al. A New Antidiabetic Agent Showing Short- and Long-Term Effects Due to Peroxisome Proliferator-Activated Receptor Alpha/Gamma Dual Agonism and Mitochondrial Pyruvate Carrier Inhibition. J Med Chem. 2023 Feb 15.  

Chemical & Physical Properties

[ Molecular Formula ]:
C25H20O3

[ Molecular Weight ]:
368.42

Related Compounds