PPARα/γ agonist 2

Modify Date: 2024-03-06 16:02:53

PPARα/γ agonist 2 Structure
PPARα/γ agonist 2 structure
Common Name PPARα/γ agonist 2
CAS Number 2213365-56-9 Molecular Weight 368.42
Density N/A Boiling Point N/A
Molecular Formula C25H20O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PPARα/γ agonist 2


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].

 Names

Name PPARα/γ agonist 2

 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
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