Eprotirome
Based on 1 Customer Validation
Eprotirome (KB2115) is a liver-selective thyroid hormone receptor (TR) agonist. KB2115 has modestly higher affinity for TRβ than for TRα. Eprotirome reduces low-density lipoprotein (LDL) cholesterol concentrations. Eprotirome can be used for dyslipidemias and obesity research.
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: 99.71%
- CAS 番号: 355129-15-6
- 分子式: C18H17Br2NO5
- 分子量:487.14
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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生物活性
Thyroid hormone receptor[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| GH3 | EC50 |
0.43 nM
Compound: 1a; KB2115
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Agonist activity at thyroid hormone receptor in rat GH3 cells expressing TRE measured after 24 hrs in presence of T3 by luciferase reporter gene assay
Agonist activity at thyroid hormone receptor in rat GH3 cells expressing TRE measured after 24 hrs in presence of T3 by luciferase reporter gene assay
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[PMID: 27120257] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 355129-15-6
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性状 Solid
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分子量 487.14
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分子式 C18H17Br2NO5
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Color White to light yellow
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SMILES
O=C(O)CC(NC1=CC(Br)=C(OC2=CC=C(O)C(C(C)C)=C2)C(Br)=C1)=O
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別名
KB2115
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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 In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 125 mg/mL (256.60 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)
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: ≥ 2.08 mg/mL (4.27 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.27 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
プロトコル
Twelve-week old male ob/ob mice are used in this study. A catheter is implanted into the right internal jugular vein before the hyperinsulinemic-euglycemic clamp. After recovery, mice are administered Eprotirome (0.3 mg/kg) via intraperitoneal injection for 10 days. On the day of the clamp experiment, conscious, overnight-fasted mice receive a primed (10 μCi) and constant rate intravenous infusion (0.1 μCi /min) of [3-3H] glucose to measure basal glucose turnover. After 60 to 75 minutes of labeled glucose infusion, the hyperinsulinemic-euglycemic clamp is performed with continuous infusion of insulin (12 mU/kg/min) and variable infusion of 25% glucose to maintain euglycemia (~120 mg/dL). Blood samples are collected by tail bleeding (approximately every 10 min) to measure blood glucose concentrations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (273 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Martagón AJ, et al. The amelioration of hepatic steatosis by thyroid hormone receptor agonists is insufficient to restore insulin sensitivity in ob/ob mice. PLoS One. 2015 Apr 7;10(4):e0122987. [Content Brief]
[2]. Rosalba Senese, et al. Thyroid hormone metabolites and analogues. Endocrine. 2019 Oct;66(1):105-114. [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 | 2.0528 mL | 10.2640 mL | 20.5280 mL | 51.3199 mL |
| 5 mM | 0.4106 mL | 2.0528 mL | 4.1056 mL | 10.2640 mL | |
| 10 mM | 0.2053 mL | 1.0264 mL | 2.0528 mL | 5.1320 mL | |
| 15 mM | 0.1369 mL | 0.6843 mL | 1.3685 mL | 3.4213 mL | |
| 20 mM | 0.1026 mL | 0.5132 mL | 1.0264 mL | 2.5660 mL | |
| 25 mM | 0.0821 mL | 0.4106 mL | 0.8211 mL | 2.0528 mL | |
| 30 mM | 0.0684 mL | 0.3421 mL | 0.6843 mL | 1.7107 mL | |
| 40 mM | 0.0513 mL | 0.2566 mL | 0.5132 mL | 1.2830 mL | |
| 50 mM | 0.0411 mL | 0.2053 mL | 0.4106 mL | 1.0264 mL | |
| 60 mM | 0.0342 mL | 0.1711 mL | 0.3421 mL | 0.8553 mL | |
| 80 mM | 0.0257 mL | 0.1283 mL | 0.2566 mL | 0.6415 mL | |
| 100 mM | 0.0205 mL | 0.1026 mL | 0.2053 mL | 0.5132 mL |
Eprotirome 関連分類
HY-10473 関連分類
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