TR antagonist 2
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].
Product Specifications
CAS Number
[1073179-55-1]
UNSPSC
12352005
Target
Thyroid Hormone Receptor
Related Pathways
Vitamin D Related/Nuclear Receptor
Field of Research
Metabolic Disease
Purity
98.94
Smiles
O=C(NC1=CC=CC(C(F)(F)F)=C1)NNC(CC2=CCN(CC2)C3=CC=C([N+]([O-])=O)C=C3)=O
Molecular Formula
C21H20F3N5O4
Molecular Weight
463.41
References & Citations
[1]Herbert H, et al. Hydrazide compounds as thyroid hormone receptor modulators and uses thereof. WO2008130637A1. 2008-10-30.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
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