Thyroid Hormone Receptor Antagonist (1-850)
目录号 : GC10413Blocks T3 binding to the thyroid hormone receptor
Cas No.:251310-57-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
| 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 |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 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。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。