TR antagonist 2 (Compound 10a) is a competitive thyroid hormone receptors (TRalpha/beta) antagonist (IC50=47 nM). TR antagonist 2 competes with triiodothyronine (T3) for binding to the ligand-binding domain of TR to block receptor-coactivator complex formation and inhibit target gene transcription, reducing thyroid hormone-mediated hypermetabolic effects. TR antagonist 2 is promising for research of hyperthyroidism (e.g., Graves disease) and thyrotoxicosis[1].
Molecular Weight:
463.41
Purity:
98.94
CAS Number:
[1073179-55-1]
Formula:
C21H20F3N5O4
Target:
Thyroid Hormone Receptor
Application Notes:
MCE Product type: Reference compound
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