1073179-55-1
Chemical Structure
TR antagonist 2
- CAS. Nr.: 1073179-55-1
- Formula:C21H20F3N5O4
- Molecular Weight:463.41
SMILES: O=C(NC1=CC=CC(C(F)(F)F)=C1)NNC(CC2=CCN(CC2)C3=CC=C([N+]([O-])=O)C=C3)=O
Biological Activity: TR antagonist 2 (Compound 10a) is a competitive thyroid hormone receptors (TRα/β) 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].
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TR antagonist 2 | 96.85% | TR antagonist 2 (Compound 10a) is a competitive thyroid hormone receptors (TRα/β) 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. | ||||||||||||||||||||
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Keywords