Berotralstat
Based on 1 publication(s) in Google Scholar
Berotralstat (BCX7353) is an orally active plasma kallikrein inhibitor. Berotralstat can reduce brain edema and is being studied for glioblastoma and hereditary angioedema.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.73%
- No. CAS: 1809010-50-1
- Fòrmula: C30H26F4N6O
- Peso molecular:562.56
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Almacenamiento:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Berotralstat
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Actividad biológica
Plasma kallikrein[1]
Berotralstat inhibits the activity of kallikrein, reduces the generation of kinin, thereby blocking kinin-mediated increased vascular permeability and edema formation. Berotralstat inhibits the proliferation and migration of glioblastoma cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Berotralstat (8 μM, single dose) inhibits plasma kallikrein activity and reduces contact pathway-initiated thrombin generation in F12+/+ or F12-/- mouse models[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:F12+/+ and F12-/- mouse models[4]
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Dosage:8 μM
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Administration:single dose
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Result:Prolonged thrombin generation lag time and decreased thrombin peak value.
Chemical Information
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No. CAS 1809010-50-1
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Appearance Solid
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Peso molecular 562.56
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Fòrmula C30H26F4N6O
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Color White to off-white
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SMILES
O=C(C1=CC(C(F)(F)F)=NN1C2=CC(CN)=CC=C2)NC3=CC([C@@H](C4=CC(C#N)=CC=C4)NCC5CC5)=CC=C3F
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Synonyms
BCX7353
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
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Blood Adv
2024 Jun 25;8(12):3045-3057. PMID: 38593231
Solvente y solubilidad
DMSO : 100 mg/mL (177.76 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 (stored under nitrogen). 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 (stored under nitrogen). 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.
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 (stored under nitrogen)
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.
Pureza y Documentación
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Ficha de datos (277 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Zuraw B, et al. Oral once-daily berotralstat for the prevention of hereditary angioedema attacks: A randomized, double-blind, placebo-controlled phase 3 trial [published online ahead of print, 2020 Oct 21]. J Allergy Clin Immunol. 2020;S0091-6749(20)31484-6. [Content Brief]
[3]. Perego F, et al., Current and emerging biologics for the treatment of hereditary angioedema. Expert Opin Biol Ther. 2019 Jun;19(6):517-526. [Content Brief]
[4]. Wan J, et al., Plasma kallikrein supports FXII-independent thrombin generation in mouse whole blood. Blood Adv. 2024 Jun 25;8(12):3045-3057. [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 (stored under nitrogen). 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 | 1.7776 mL | 8.8879 mL | 17.7759 mL | 44.4397 mL |
| 5 mM | 0.3555 mL | 1.7776 mL | 3.5552 mL | 8.8879 mL | |
| 10 mM | 0.1778 mL | 0.8888 mL | 1.7776 mL | 4.4440 mL | |
| 15 mM | 0.1185 mL | 0.5925 mL | 1.1851 mL | 2.9626 mL | |
| 20 mM | 0.0889 mL | 0.4444 mL | 0.8888 mL | 2.2220 mL | |
| 25 mM | 0.0711 mL | 0.3555 mL | 0.7110 mL | 1.7776 mL | |
| 30 mM | 0.0593 mL | 0.2963 mL | 0.5925 mL | 1.4813 mL | |
| 40 mM | 0.0444 mL | 0.2222 mL | 0.4444 mL | 1.1110 mL | |
| 50 mM | 0.0356 mL | 0.1778 mL | 0.3555 mL | 0.8888 mL | |
| 60 mM | 0.0296 mL | 0.1481 mL | 0.2963 mL | 0.7407 mL | |
| 80 mM | 0.0222 mL | 0.1111 mL | 0.2222 mL | 0.5555 mL | |
| 100 mM | 0.0178 mL | 0.0889 mL | 0.1778 mL | 0.4444 mL |
Berotralstat Related Classifications
HY-109127 Related Classifications
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