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Thyroid Hormone Receptor Antagonist (1-850)

目录号 : GC10413

Blocks T3 binding to the thyroid hormone receptor

Thyroid Hormone Receptor Antagonist (1-850) Chemical Structure

Cas No.:251310-57-3

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1mg
¥634.00
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5mg
¥2,491.00
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10mg
¥4,647.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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.

Chemical Properties

Cas No. 251310-57-3 SDF
化学名 2-[1-(4-nitrophenyl)-4-piperidinylidene]-acetic acid-2-[[[3-(trifluoromethyl)phenyl]amino]carbonyl]hydrazide
Canonical SMILES O=C(NNC(/C=C1CCN(C2=CC=C([N+]([O-])=O)C=C2)CC/1)=O)NC3=CC(C(F)(F)F)=CC=C3
分子式 C21H20F3N5O4 分子量 463.4
溶解度 ≤0.5mg/ml in ethanol;50mg/ml in DMSO;50mg/ml in dimethyl formamide 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.158 mL 10.7898 mL 21.5796 mL
5 mM 0.4316 mL 2.158 mL 4.3159 mL
10 mM 0.2158 mL 1.079 mL 2.158 mL
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