Bretazenil
Based on 1 Customer Validation
Bretazenil (Ro 16-6028) is a partial agonist at the gamma-aminobutyric acid A (GABAA) receptor-linked benzodiazepine site. Bretazenil is potent benzodiazepine examined, exhibiting an IC50 (concentration at which half-maximal inhibition of specific [35S]TBPS binding occurs) of 6.1 nM. Bretazenil shows an EC50 of 10 nM for recombinant α1β1γ2. Anticonvulsant effects.
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- Purity: 99.13%
- CAS No.: 84379-13-5
- 화학식: C19H20BrN3O3
- 분자량:418.28
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 84379-13-5
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Appearance Solid
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분자량 418.28
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화학식 C19H20BrN3O3
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Color White to off-white
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SMILES
CC(C)(C)OC(C1=C2N(C=N1)C3=CC=CC(Br)=C3C(N4[C@@]2([H])CCC4)=O)=O
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Synonyms
Ro 16-6028
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 50 mg/mL (119.54 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. 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (5.98 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 (5.98 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.
순도&문서
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Data Sheet (282 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Puia G, et al. Molecular mechanisms of the partial allosteric modulatory effects of bretazenil at gamma-aminobutyric acid type A receptor. Proc Natl Acad Sci U S A. 1992;89(8):3620-3624. [Content Brief]
[2]. Finn DA, et al. A comparison of Ro 16-6028 with benzodiazepine receptor 'full agonists' on GABAA receptor function. Eur J Pharmacol. 1993;247(3):233-237. [Content Brief]
[3]. Kubová H, et al. Anticonvulsant effects of bretazenil (Ro 16-6028) during ontogenesis. Epilepsia. 1993;34(6):1130-1134. [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 | 2.3907 mL | 11.9537 mL | 23.9074 mL | 59.7686 mL |
| 5 mM | 0.4781 mL | 2.3907 mL | 4.7815 mL | 11.9537 mL | |
| 10 mM | 0.2391 mL | 1.1954 mL | 2.3907 mL | 5.9769 mL | |
| 15 mM | 0.1594 mL | 0.7969 mL | 1.5938 mL | 3.9846 mL | |
| 20 mM | 0.1195 mL | 0.5977 mL | 1.1954 mL | 2.9884 mL | |
| 25 mM | 0.0956 mL | 0.4781 mL | 0.9563 mL | 2.3907 mL | |
| 30 mM | 0.0797 mL | 0.3985 mL | 0.7969 mL | 1.9923 mL | |
| 40 mM | 0.0598 mL | 0.2988 mL | 0.5977 mL | 1.4942 mL | |
| 50 mM | 0.0478 mL | 0.2391 mL | 0.4781 mL | 1.1954 mL | |
| 60 mM | 0.0398 mL | 0.1992 mL | 0.3985 mL | 0.9961 mL | |
| 80 mM | 0.0299 mL | 0.1494 mL | 0.2988 mL | 0.7471 mL | |
| 100 mM | 0.0239 mL | 0.1195 mL | 0.2391 mL | 0.5977 mL |
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