TR antagonist 2 - CAS 1073179-55-1

TR antagonist 2 (Compound 10a) is a competitive inhibitor of thyroid hormone receptors (TRα/β) with an IC50 of 47 nM. It works by competitively binding to the ligand-binding domain of the receptor with triiodothyronine (T3), thereby blocking the formation of the receptor-coactivator complex, inhibiting target gene transcription, and reducing thyroid hormone-mediated metabolic effects. TR antagonist 2 holds potential for research into hyperthyroidism (such as Graves' disease) and thyrotoxicosis.

Thyroid hormone receptor (THR)

Endocrinology/Hormones

1073123

C21H20F3N5O4

463.41

O=C(NNC(=O)CC1=CCN(C2=CC=C(C=C2)N(=O)=O)CC1)NC3=CC=CC(=C3)C(F)(F)F

-20°C

Ice Packs

Small Compound