251310-57-3
Chemical Structure
Thyroid hormone receptor antagonist (1-850)
- CAS No.: 251310-57-3
- Formula:C21H20F3N5O4
- Molecular Weight:463.41
IUPAC Name: 2-(2-(1-(4-nitrophenyl)piperidin-4-ylidene)acetyl)-N-(3-(trifluoromethyl)phenyl)hydrazine-1-carboxamide
InChIKey: CZMAYVNXNKBQKX-UHFFFAOYSA-N
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
Biological Activity: 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].
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Thyroid hormone receptor antagonist (1-850) | 99.04% | 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. | ||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]