| CAS NO: | 251310-57-3 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 463.4 |
| Cas No. | 251310-57-3 |
| Formula | C21H20F3N5O4 |
| Solubility | ≤0.5mg/ml in ethanol;50mg/ml in DMSO;50mg/ml in dimethyl formamide |
| Chemical Name | 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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.
m.cnreagent.com