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DS45500853 Sale

目录号 : GC64533

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。

DS45500853 Chemical Structure

Cas No.:2735803-28-6

规格 价格 库存 购买数量
5 mg
¥2,250.00
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10 mg
¥3,600.00
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25 mg
¥7,650.00
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50 mg
¥12,150.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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.

Chemical Properties

Cas No. 2735803-28-6 SDF Download SDF
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) 储存条件 Store at -20°C
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1 mM 3.5168 mL 17.584 mL 35.1679 mL
5 mM 0.7034 mL 3.5168 mL 7.0336 mL
10 mM 0.3517 mL 1.7584 mL 3.5168 mL
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Research Update

Discovery of a Novel Class of ERRα Agonists

ACS Med Chem Lett 2021 Apr 21;12(5):817-821.PMID:34055231DOI:PMC8155236

A novel class of estrogen-related receptor α (ERRα) agonists has been discovered. A structure-activity relationship study of high-throughput screening hits 1 and 2 led to the discovery of benzimidazole 3d (DS20362725) and acetophenone analogue 5c (DS45500853). The X-ray crystal structure of the ERRα ligand-binding domain in complex with 5c and PGC-1α coactivator peptide revealed conformational changes in the ligand-binding pocket to accommodate 5c and the key interaction between the protein and ligand. Since both analogues avoided PPARγ transcriptional activity, they can be useful tool compounds for investigating biological ERRα functions.