ERRγ inverse agonist 1 

ERRγ inverse agonist 1 (Compound 12) is a selective ERRγ inverse agonist with an IC₅₀ value of 0.040 μM against ERRγ. ERRγ inverse agonist 1 inhibits the activity of ERRγ at the functional level. ERRγ inverse agonist 1 can be used in the research of anaplastic thyroid cancer^[1].

ERRγ inverse agonist 1 potently inhibits the binding of ERRγ in a cell-free TR-FRET assay, with an IC₅₀ of 0.040 μM^[1].
ERRγ inverse agonist 1 (10 μM; 15 min) inhibits the activities of CYP 2D6 and CYP 3A4 by 36.5% and 33.6%, respectively, in in vitro microsomal assays, while exerting extremely weak inhibitory effects on other tested CYP subtypes^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

529.54

C₃₀H₃₈Cl₂N₂O₂

2316832-86-5

OC1=CC=CC(/C(C2=CC=C(N3CCN(C(C)C)CC3)C=C2)=C(C4=CC=CC=C4)\CCCO)=C1.[H]Cl.[H]Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Kim J, et al. Discovery of Potent, Selective, and Orally Bioavailable Estrogen-Related Receptor-γ Inverse Agonists To Restore the Sodium Iodide Symporter Function in Anaplastic Thyroid Cancer. J Med Chem. 2019;62(4):1837-1858.  [Content Brief]