ERRγ agonist-2

Names

[ CAS No. ]:
324022-01-7

[ Name ]:
ERRγ agonist-2

Biological Activity

[Description]:

ERRγ agonist-2 is a potent and selective ERRγ inverse agonist with a Kd value of 6.5 μM. ERRγ agonist-2 inhibits the expression of hepcidin, fibrinogen and gluconeogenic genes. ERRγ agonist-2 has antimicrobial, anti-coagulant and antidiabetic activities[1].

[Related Catalog]:

Signaling Pathways >> Others >> Estrogen Receptor/ERR
Research Areas >> Infection
Research Areas >> Metabolic Disease

[Target]

ERRγ:6.5 μM (Kd)


[In Vitro]

ERRγ agonist-2 (1-10 μM; 293T 细胞) 抑制 ERRγ 的 PGC-1α 依赖性转录活性，对 ERRα 和 ERRβ 的抑制作用微弱[1]。 ERRγ agonist-2 (10 μM; AML12 细胞) 抑制铁调素、纤维蛋白原和糖异生基因的表达[1]。

[References]

[1]. Yang SH, et, al. Structure-based discovery of pyrazolamides as novel ERRγ inverse agonists. Eur J Med Chem. 2023 Mar 15;250:115174.  

Chemical & Physical Properties

[ Molecular Formula ]:
C27H21N5O2

[ Molecular Weight ]:
447.49

Related Compounds

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