Berotralstat dihydrochloride
Based on 1 publication(s) in Google Scholar
Berotralstat dihydrochloride (BCX7353 dihydrochloride) is an orally active plasma kallikrein inhibitor. Berotralstat can reduce brain edema and is being studied for glioblastoma and hereditary angioedema.
For research use only. We do not sell to patients.
- Purity: 98.67%
- CAS No.: 1809010-52-3
- Formula: C30H28Cl2F4N6O
- Molecular Weight:635.48
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Storage:
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Berotralstat dihydrochloride
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Biological Activity
Berotralstat dihydrochloride inhibits the activity of kallikrein, reduces the generation of kinin, thereby blocking kinin-mediated increased vascular permeability and edema formation. Berotralstat dihydrochloride 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 dihydrochloride (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..
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1809010-52-3
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Appearance Solid
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Molecular Weight 635.48
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Formula C30H28Cl2F4N6O
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Color Off-white to light yellow
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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.[H]Cl.[H]Cl
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Synonyms
BCX7353 dihydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
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
Solvent & Solubility
DMSO : 120 mg/mL (188.83 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, 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 (stored under nitrogen, 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.
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: ≥ 1.2 mg/mL (1.89 mM); Clear solution
This protocol yields a clear solution of ≥ 1.2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.0 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: ≥ 1.2 mg/mL (1.89 mM); Clear solution
This protocol yields a clear solution of ≥ 1.2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.0 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 (stored under nitrogen, 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.
Purity & Documentation
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Data Sheet (276 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)
References
[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, 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 |
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| DMSO | 1 mM | 1.5736 mL | 7.8681 mL | 15.7361 mL | 39.3403 mL |
| 5 mM | 0.3147 mL | 1.5736 mL | 3.1472 mL | 7.8681 mL | |
| 10 mM | 0.1574 mL | 0.7868 mL | 1.5736 mL | 3.9340 mL | |
| 15 mM | 0.1049 mL | 0.5245 mL | 1.0491 mL | 2.6227 mL | |
| 20 mM | 0.0787 mL | 0.3934 mL | 0.7868 mL | 1.9670 mL | |
| 25 mM | 0.0629 mL | 0.3147 mL | 0.6294 mL | 1.5736 mL | |
| 30 mM | 0.0525 mL | 0.2623 mL | 0.5245 mL | 1.3113 mL | |
| 40 mM | 0.0393 mL | 0.1967 mL | 0.3934 mL | 0.9835 mL | |
| 50 mM | 0.0315 mL | 0.1574 mL | 0.3147 mL | 0.7868 mL | |
| 60 mM | 0.0262 mL | 0.1311 mL | 0.2623 mL | 0.6557 mL | |
| 80 mM | 0.0197 mL | 0.0984 mL | 0.1967 mL | 0.4918 mL | |
| 100 mM | 0.0157 mL | 0.0787 mL | 0.1574 mL | 0.3934 mL |
Berotralstat dihydrochloride Related Classifications
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