RXR antagonist 1
Based on 1 Customer Validation
RXR antagonist 1 (compound 6a) is a retinoid X receptor (RXR) modulator. RXR antagonist 1 shows potent RXR-antagonistic activity, with a pA2 of 8.06. RXR antagonist 1 can be used for type 2 diabetes research.
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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: 99.94%
- CAS 番号: 3010910-40-1
- 分子式: C28H33F3N2O3
- 分子量:502.57
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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
RXR antagonist 1 (compound 6a) shows potent RXR-antagonistic activities at 1 μM[1].
RXR antagonist 1 shows competitive binding to the LBP in hRXRα-LBD, with Ki of 0.384 ± 0.072, Kd of 0.277 ± 0.038, and Ki/Kd of 1.39[1].
The cell permeability of RXR antagonist 1 shows no correlation with RXR-antagonistic activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 3010910-40-1
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性状 Solid
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分子量 502.57
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分子式 C28H33F3N2O3
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Color White to off-white
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SMILES
CCCCCOC1=CC2=C(C(C)(CCC2(C)C)C)C=C1N3C(C(F)(F)F)=NC4=C3C=CC(C(O)=O)=C4
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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
DMSO : 100 mg/mL (198.98 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: 2.5 mg/mL (4.97 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
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.
純度とドキュメンテーション
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データシート (277 KB)
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SDS (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 | 1.9898 mL | 9.9489 mL | 19.8977 mL | 49.7443 mL |
| 5 mM | 0.3980 mL | 1.9898 mL | 3.9795 mL | 9.9489 mL | |
| 10 mM | 0.1990 mL | 0.9949 mL | 1.9898 mL | 4.9744 mL | |
| 15 mM | 0.1327 mL | 0.6633 mL | 1.3265 mL | 3.3163 mL | |
| 20 mM | 0.0995 mL | 0.4974 mL | 0.9949 mL | 2.4872 mL | |
| 25 mM | 0.0796 mL | 0.3980 mL | 0.7959 mL | 1.9898 mL | |
| 30 mM | 0.0663 mL | 0.3316 mL | 0.6633 mL | 1.6581 mL | |
| 40 mM | 0.0497 mL | 0.2487 mL | 0.4974 mL | 1.2436 mL | |
| 50 mM | 0.0398 mL | 0.1990 mL | 0.3980 mL | 0.9949 mL | |
| 60 mM | 0.0332 mL | 0.1658 mL | 0.3316 mL | 0.8291 mL | |
| 80 mM | 0.0249 mL | 0.1244 mL | 0.2487 mL | 0.6218 mL | |
| 100 mM | 0.0199 mL | 0.0995 mL | 0.1990 mL | 0.4974 mL |