1'-Hydroxy bufuralol
Based on 1 Customer Validation
1'-Hydroxy bufuralol is the main metabolite of Bufuralol (HY-105124) by the cytochrome P450 isoenzymes 2D1 and 2D2 (CYP2D1/2). 1'-Hydroxy bufuralol can be used to determine CYP2D1/2 enzyme activity.
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- Reinheit: 96.62%
- CAS. Nr.: 57704-16-2
- Formel: C16H23NO3
- Molecular Weight:277.36
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Speicherung:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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CYP2 |
Bufuralol is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol is widely used in the characterization of CYP2D6 activity, and possesses aromatic rings and a basic nitrogen that are characteristic of CYP2D6 substrates.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 57704-16-2
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Appearance <41°C Solid,>49°C Liquid
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Molecular Weight 277.36
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Formel C16H23NO3
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Color Off-white to light yellow
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SMILES
CC(C1=C2OC(C(CNC(C)(C)C)O)=CC2=CC=C1)O
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Synonyms
Ro 03-7410
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (360.54 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 5 mg/mL (18.03 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (18.03 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Reinheit & Dokumentation
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Data Sheet (274 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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Handling Instructions (2659 KB)
Verweise
[1]. Evangelos P Daskalopoulos, et al. D₂-dopaminergic receptor-linked pathways: critical regulators of CYP3A, CYP2C, and CYP2D. Mol Pharmacol. 2012 Oct;82(4):668-78. [Content Brief]
[2]. H Yamazaki, et al. Bufuralol hydroxylation by cytochrome P450 2D6 and 1A2 enzymes in human liver microsomes. Mol Pharmacol. 1994 Sep;46(3):568-77. [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 (sealed storage, away from moisture). 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 | 3.6054 mL | 18.0271 mL | 36.0542 mL | 90.1356 mL |
| 5 mM | 0.7211 mL | 3.6054 mL | 7.2108 mL | 18.0271 mL | |
| 10 mM | 0.3605 mL | 1.8027 mL | 3.6054 mL | 9.0136 mL | |
| 15 mM | 0.2404 mL | 1.2018 mL | 2.4036 mL | 6.0090 mL | |
| 20 mM | 0.1803 mL | 0.9014 mL | 1.8027 mL | 4.5068 mL | |
| 25 mM | 0.1442 mL | 0.7211 mL | 1.4422 mL | 3.6054 mL | |
| 30 mM | 0.1202 mL | 0.6009 mL | 1.2018 mL | 3.0045 mL | |
| 40 mM | 0.0901 mL | 0.4507 mL | 0.9014 mL | 2.2534 mL | |
| 50 mM | 0.0721 mL | 0.3605 mL | 0.7211 mL | 1.8027 mL | |
| 60 mM | 0.0601 mL | 0.3005 mL | 0.6009 mL | 1.5023 mL | |
| 80 mM | 0.0451 mL | 0.2253 mL | 0.4507 mL | 1.1267 mL | |
| 100 mM | 0.0361 mL | 0.1803 mL | 0.3605 mL | 0.9014 mL |
1'-Hydroxy bufuralol Related Classifications
HY-122277 Related Classifications
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