1. Vitamin D Related/Nuclear Receptor
  2. Thyroid Hormone Receptor
  3. 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.

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TR antagonist 2 Chemical Structure

TR antagonist 2 Chemical Structure

CAS No. : 1073179-55-1

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Description

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].

Molecular Weight

463.41

Formula

C21H20F3N5O4

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1=CC=CC(C(F)(F)F)=C1)NNC(CC2=CCN(CC2)C3=CC=C([N+]([O-])=O)C=C3)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
TR antagonist 2
Cat. No.:
HY-127024A
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