TR antagonist 2

• Target:

  Thyroid hormone receptor (THR)

• Related Pathways:

  Endocrinology/Hormones

• Bioactivity:

  TR antagonist 2 (Compound 10a) is a competitive inhibitor of thyroid hormone receptors (TR?/?) 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.

• Smiles:

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

• Molecular Formula:

  C21H20F3N5O4

• Molecular Weight:

  463.41

• Shipping Conditions:

  Cool pack

• Storage Temperature:

  -20°C

• CAS Number:

  1073179-55-1