Thyroid hormone receptor antagonist (1-850)

Thyroid hormone receptor antagonist (1-850) is a competitive, selective and high-affinity thyroid hormone receptor (TR) antagonist with an IC50 of 1.5 μM for antagonizing the effect of T3 on TR. Thyroid hormone receptor antagonist (1-850) blocks T3-mediated interaction of TRα and TRβ with nuclear receptor coactivator. Thyroid hormone receptor antagonist (1-850) has no effect on the activity of RARα[1][2][3].

Product Specifications

CAS Number

[251310-57-3]

UNSPSC

12352005

Hazard Statement

H315, H319, H320

Target

Thyroid Hormone Receptor

Type

Reference compound

Related Pathways

Vitamin D Related/Nuclear Receptor

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/thyroid-hormone-receptor-antagonist-1-850.html

Purity

99.04

Solubility

DMSO : 100 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(NC1=CC(C(F)(F)F)=CC=C1)NNC(/C=C2CCN(CC\2)C3=CC=C(C=C3)[N+]([O-])=O)=O

Molecular Formula

C21H20F3N5O4

Molecular Weight

463.41

Precautions

H315, H319, H320

References & Citations

[1]Matthieu Schapira, et al. Discovery of diverse thyroid hormone receptor antagonists by high-throughput docking. Proc Natl Acad Sci U S A. 2003 Jun 10;100 (12) :7354-9. |[2]Mercedes Fernández, et al. Thyroid Hormone Signaling in Embryonic Stem Cells: Crosstalk with the Retinoic Acid Pathway. Int J Mol Sci. 2020 Nov 25;21 (23) :8945.|[3]Pamela Navarrete-Ramírez, et al. 3,5-di-iodothyronine stimulates tilapia growth through an alternate isoform of thyroid hormone receptor β1. J Mol Endocrinol. 2014 Feb 1;52 (1) :1-9.