Thyroid Hormone Receptor Antagonist (1-850) |
| Catalog No.GC10413 |
Thyroid hormone receptor antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 251310-57-3
Sample solution is provided at 25 µL, 10mM.
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Target: thyroid hormone receptor
IC50: 1.5 μM
Thyroid hormone receptor antagonist (1-850) was screened from a library of more than 250000 compounds as the antagonist of thyroid hormone receptor with the highest affinity. Thyroid Hormone Receptor Antagonist, 1-850 is a cell-permeable hydrazinyl-carboxamide compound which functions as a selective and high-affinity thyroid receptor antagonist with the IC50 value of 1.5 μM in Hela cells [1].
The thyroid hormone receptor (TR) is a type of nuclear receptor that is activated by binding thyroid hormone, which plays a critical role in the regulation of metabolism and heart rate and the development of organisms. Thyroid hormone receptor antagonist (1-850) could competitively block T3 (L-triiodothyronine) binding to both TRα and TRβ, and suppress T3 mediated interaction of TRα with nuclear receptor coactivator (NRC) as well as prevent the stimulation of gene expression [1].
In Vitro: no data available.
In Vivo: no data available.
Clinical trial: no data available.
Reference:
[1] Schapira M, Raaka B M, Das S, et al. Discovery of diverse thyroid hormone receptor antagonists by high-throughput docking[J]. Proceedings of the National Academy of Sciences of the United States of America, 2003, 100(12): 7354-7359.
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