TR antagonist 2
Based on 1 Customer Validation
TR antagonist 2 (Compound 10a) is a competitive thyroid hormone receptors (TRα/β) antagonist (IC50=47 nM). TR antagonist 2 competes with triiodothyronine (T3) for binding to the ligand-binding domain of TR to block receptor-coactivator complex formation and inhibit target gene transcription, reducing thyroid hormone-mediated hypermetabolic effects. TR antagonist 2 is promising for research of hyperthyroidism (e.g., Graves' disease) and thyrotoxicosis.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 96.85%
- CAS 番号: 1073179-55-1
- 分子式: C21H20F3N5O4
- 分子量:463.41
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
製品説明
化学情報
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CAS 番号 1073179-55-1
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性状 Solid
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分子量 463.41
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分子式 C21H20F3N5O4
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Color Light yellow to yellow
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SMILES
O=C(NC1=CC=CC(C(F)(F)F)=C1)NNC(CC2=CCN(CC2)C3=CC=C([N+]([O-])=O)C=C3)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 50 mg/mL (107.90 mM; Need ultrasonic; 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
純度とドキュメンテーション
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データシート (268 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
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 |