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Thyroid Hormone Receptor Antagonist(1-850)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Thyroid Hormone Receptor Antagonist(1-850)图片
CAS NO:251310-57-3
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
Cas No.251310-57-3
化学名2-[1-(4-nitrophenyl)-4-piperidinylidene]-acetic acid-2-[[[3-(trifluoromethyl)phenyl]amino]carbonyl]hydrazide
Canonical SMILESO=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
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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.