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].

Thyroid hormone receptor antagonist (1-850) (10 μM；持续 7 天) 消除 Retinoic Acid (RA；HY-14649；1 μM) 诱导的巢蛋白 mRNA 表达增加^[2]。
Thyroid hormone receptor antagonist (1-850) (0.1-20 μM；24 小时) 可有效阻断器官型罗非鱼肝脏培养物中 IGF1 mRNA 表达，同时增加 D2 mRNA 表达^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

463.41

C₂₁H₂₀F₃N₅O₄

251310-57-3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]