| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | DS45500853 | ||||||||||||
| CAS | 2735803-28-6 | ||||||||||||
| Formula | C18H20O3 | ||||||||||||
| Molar Mass | 284.35 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Shinozuka T, et al. Discovery of a Novel Class of ERRα Agonists. ACS Med Chem Lett. 2021 Apr 21;12(5):817-821. |