Bupranolol
Based on 1 Customer Validation
Bupranolol is an orally active, competitive and non-selective β-adrenoceptor antagonist without intrinsic sympathomimetic activity.
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: 98.73%
- CAS 番号: 14556-46-8
- 分子式: C14H22ClNO2
- 分子量:271.78
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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
Adrenergic Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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β-adrenoceptor |
Bupranolol (1~3 μM) shifts isoprenaline-induced relaxation in the presence of 30 μM propranolol. Bupranolol acts as a competitive antagonist of isoprenaline-induced relaxation in the presence of 300 nM propranolol, with a pA2 value of 5.90. Bupranolol antagonizes β1- and β2-ARs with pA2 values of ≈9.0, and also antagonizes β3-AR with a pA2 value of 6.0[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 14556-46-8
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性状 Solid
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分子量 271.78
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分子式 C14H22ClNO2
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Color White to off-white
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SMILES
OC(CNC(C)(C)C)COC1=CC(C)=CC=C1Cl
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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 : 50 mg/mL (183.97 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.
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 (9.20 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.20 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 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.
純度とドキュメンテーション
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データシート (271 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Chino D, et al. Pharmacological identification of β-adrenoceptor subtypes mediating isoprenaline-induced relaxation of guinea pig colonic longitudinal smooth muscle. J Smooth Muscle Res. 2018;54(0):13-27. [Content Brief]
[2]. Babu RJ, et al. Effect of cyclodextrins on the complexation and transdermal delivery of bupranolol through rat skin. Int J Pharm. 2004;271(1-2):155-165. [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 | 3.6794 mL | 18.3972 mL | 36.7945 mL | 91.9862 mL |
| 5 mM | 0.7359 mL | 3.6794 mL | 7.3589 mL | 18.3972 mL | |
| 10 mM | 0.3679 mL | 1.8397 mL | 3.6794 mL | 9.1986 mL | |
| 15 mM | 0.2453 mL | 1.2265 mL | 2.4530 mL | 6.1324 mL | |
| 20 mM | 0.1840 mL | 0.9199 mL | 1.8397 mL | 4.5993 mL | |
| 25 mM | 0.1472 mL | 0.7359 mL | 1.4718 mL | 3.6794 mL | |
| 30 mM | 0.1226 mL | 0.6132 mL | 1.2265 mL | 3.0662 mL | |
| 40 mM | 0.0920 mL | 0.4599 mL | 0.9199 mL | 2.2997 mL | |
| 50 mM | 0.0736 mL | 0.3679 mL | 0.7359 mL | 1.8397 mL | |
| 60 mM | 0.0613 mL | 0.3066 mL | 0.6132 mL | 1.5331 mL | |
| 80 mM | 0.0460 mL | 0.2300 mL | 0.4599 mL | 1.1498 mL | |
| 100 mM | 0.0368 mL | 0.1840 mL | 0.3679 mL | 0.9199 mL |