1. Vitamin D Related/Nuclear Receptor
  2. Estrogen Receptor/ERR
  3. 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.

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ERRγ inverse agonist 1

ERRγ inverse agonist 1 Estructura química

No. CAS : 2316832-86-5

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Descripciòn

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].

IC50 & Target[1]

ERRγ

0.040 μM (IC50)

ERRβ

1.330 μM (IC50)

ERα

1.240 μM (IC50)

In Vitro

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.

Peso molecular

529.54

Fòrmula

C30H38Cl2N2O2

No. CAS
SMILES

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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

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Nombre del producto:
ERRγ inverse agonist 1
Cat. No.:
HY-114411
Cantidad:
MCE Japan Authorized Agent: