Thyroid hormone receptor antagonist (1-850)
Based on 1 Customer Validation
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.
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- Pureza : 99.04%
- No. CAS: 251310-57-3
- Fòrmula: C21H20F3N5O4
- Peso molecular:463.41
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
In Vitro
Thyroid hormone receptor antagonist (1-850) (10 μM; for 7 days) abolishes the increase in the expression of nestin mRNA induced by Retinoic Acid (RA; HY-14649; 1 μM) [2].
Thyroid hormone receptor antagonist (1-850) (0.1-20 μM; 24 h) effectively blocks IGF1 mRNA expression while increases D2 mRNA expression in Organotypic tilapia liver cultures[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 251310-57-3
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Appearance Solid
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Peso molecular 463.41
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Fòrmula C21H20F3N5O4
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Color Light yellow to yellow
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SMILES
O=C(NC1=CC(C(F)(F)F)=CC=C1)NNC(/C=C2CCN(CC\2)C3=CC=C(C=C3)[N+]([O-])=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (215.79 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.39 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (270 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1579 mL | 10.7896 mL | 21.5792 mL | 53.9479 mL |
| 5 mM | 0.4316 mL | 2.1579 mL | 4.3158 mL | 10.7896 mL | |
| 10 mM | 0.2158 mL | 1.0790 mL | 2.1579 mL | 5.3948 mL | |
| 15 mM | 0.1439 mL | 0.7193 mL | 1.4386 mL | 3.5965 mL | |
| 20 mM | 0.1079 mL | 0.5395 mL | 1.0790 mL | 2.6974 mL | |
| 25 mM | 0.0863 mL | 0.4316 mL | 0.8632 mL | 2.1579 mL | |
| 30 mM | 0.0719 mL | 0.3597 mL | 0.7193 mL | 1.7983 mL | |
| 40 mM | 0.0539 mL | 0.2697 mL | 0.5395 mL | 1.3487 mL | |
| 50 mM | 0.0432 mL | 0.2158 mL | 0.4316 mL | 1.0790 mL | |
| 60 mM | 0.0360 mL | 0.1798 mL | 0.3597 mL | 0.8991 mL | |
| 80 mM | 0.0270 mL | 0.1349 mL | 0.2697 mL | 0.6743 mL | |
| 100 mM | 0.0216 mL | 0.1079 mL | 0.2158 mL | 0.5395 mL |
Thyroid hormone receptor antagonist (1-850) Related Classifications
HY-127024 Related Classifications
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