DS45500853 是一种雌激素相关受体 α (ERRα) 激动剂。DS45500853 抑制受体相互作用蛋白 140 (RIP140) 辅助阻遏肽 (10 nM) 和 GST-ERRα 配体结合结构域 (LBD; 1.2 μM) 之间的结合，IC50 值为 0.80 μM。DS45500853 可用于代谢紊乱研究，如 2 型糖尿病。
货号:ajcx37800
CAS:2735803-28-6
分子式:C18H20O3
分子量：284.35
溶解度:DMSO : 50 mg/mL (175.84 mM; ultrasonic and warming and heat to 60°C)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

DS45500853 is an estrogen-related receptor α (ERRα) agonist. DS45500853 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.80 μM. DS45500853 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM)[1].

DS45500853 (compound 5c; 0.002, 0.006, 0.017, 0.051, 0.015, 0.046, 1.4, 4.2, 12.5 μg/mL; 18 h) inhibits the transcriptional activity of full-length ERRα in MG63 cells with an EC50 of 5.4 μM[1].
DS45500853 binds in the ligand-binding pocket (LBP) of the ERRα LBD as inverse agonist II[1].

[1]. Shinozuka T, et al. Discovery of a Novel Class of ERRα Agonists. ACS Med Chem Lett. 2021 Apr 21;12(5):817-821.