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DS45500853, an estrogen-related receptor α (ERRα) agonist, acts as an inhibitor of the binding interaction between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM), exhibiting an IC50 of 0.80 μM. This compound holds potential for research pertaining to metabolic disorders, particularly type 2 diabetes mellitus (T2DM).
Description | DS45500853, an estrogen-related receptor α (ERRα) agonist, acts as an inhibitor of the binding interaction between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM), exhibiting an IC50 of 0.80 μM. This compound holds potential for research pertaining to metabolic disorders, particularly type 2 diabetes mellitus (T2DM). |
In vitro | DS45500853 (compound 5c; concentrations of 0.002, 0.006, 0.017, 0.051, 0.015, 0.046, 1.4, 4.2, 12.5 μg/mL; incubation time: 18 h) effectively suppresses the transcriptional activity of full-length ERRα in MG63 cells, achieving an EC50 value of 5.4 μM[1]. This compound also acts as an inverse agonist II, specifically interacting with the ligand-binding pocket (LBP) of the ERRα LBD[1]. |
Molecular Weight | 284.355 |
Formula | C18H20O3 |
Cas No. | 2735803-28-6 |
Relative Density. | 1.107 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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