Avoralstat
Based on 5 publication(s) in Google Scholar
Avoralstat (BCX4161), a potent and orally active plasma kallikrein (PKK) inhibitor, is used for hereditary angioedema research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 97.00%
- No. CAS: 918407-35-9
- Fòrmula: C28H27N5O5
- Peso molecular:513.54
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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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
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Publications Citing Use of MedChemExpress (MCE) Avoralstat
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Actividad biológica
C1 inhibitor (C1INH) is the primary regulator of contact activation, both by inhibiting the conversion of prekallikrein to plasma kallikrein (PKK) by FXIIa, and by directly inhibiting PKK. PKK cleaves high molecular weight kininogen, releasing bradykinin, whose actions are responsible for the signs and symptoms of hereditary angioedema (HAE)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 918407-35-9
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Appearance Solid
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Peso molecular 513.54
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Fòrmula C28H27N5O5
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Color White to yellow
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SMILES
O=C(C1=NC(C(NCC2CC2)=O)=CC=C1C3=CC(OC)=C(C=C)C=C3C(NC4=CC=C(C(N)=N)C=C4)=O)O
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Synonyms
BCX4161
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (5)
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Journal Impact Factor
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Most Recent
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Circulation
Ablation of Plasma Prekallikrein Decreases Low-Density Lipoprotein Cholesterol by Stabilizing Low-Density Lipoprotein Receptor and Protects Against Atherosclerosis. [Abstract]2022 Mar;145(9):675-687. PMID: 35189703 -
J Clin Invest
Structure-based phylogeny identifies avoralstat as a TMPRSS2 inhibitor that prevents SARS-CoV-2 infection in mice. [Abstract]2021 May 17;131(10):e147973. PMID: 33844653 -
Sci Rep
Production and characterization of gigastasin, a leech-derived inhibitor of complement and coagulation pathways. [Abstract]2026 May 16. PMID: 42143157 -
J Biomol Struct Dyn
In silico and in vitro assays reveal potential inhibitors against 3CL pro main protease of SARS-CoV-2. [Abstract]2022;40(23):12800-12811. PMID: 34550861 -
Solvente y solubilidad
DMSO : 50 mg/mL (97.36 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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 (4.87 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.
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.
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]. Aygoren-Pursun E, et al. Prophylaxis of hereditary angioedema attacks: A randomized trial of oral plasma kallikrein inhibition with avoralstat. J Allergy Clin Immunol. 2016 Sep;138(3):934-936.e5. [Content Brief]
[2]. Cornpropst M, et al. Safety, pharmacokinetics, and pharmacodynamics of avoralstat, an oral plasma kallikrein inhibitor: phase 1 study. Allergy. 2016;71(12):1676-1683. [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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9473 mL | 9.7363 mL | 19.4727 mL | 48.6817 mL |
| 5 mM | 0.3895 mL | 1.9473 mL | 3.8945 mL | 9.7363 mL | |
| 10 mM | 0.1947 mL | 0.9736 mL | 1.9473 mL | 4.8682 mL | |
| 15 mM | 0.1298 mL | 0.6491 mL | 1.2982 mL | 3.2454 mL | |
| 20 mM | 0.0974 mL | 0.4868 mL | 0.9736 mL | 2.4341 mL | |
| 25 mM | 0.0779 mL | 0.3895 mL | 0.7789 mL | 1.9473 mL | |
| 30 mM | 0.0649 mL | 0.3245 mL | 0.6491 mL | 1.6227 mL | |
| 40 mM | 0.0487 mL | 0.2434 mL | 0.4868 mL | 1.2170 mL | |
| 50 mM | 0.0389 mL | 0.1947 mL | 0.3895 mL | 0.9736 mL | |
| 60 mM | 0.0325 mL | 0.1623 mL | 0.3245 mL | 0.8114 mL | |
| 80 mM | 0.0243 mL | 0.1217 mL | 0.2434 mL | 0.6085 mL |
Avoralstat Related Classifications
HY-16735 Related Classifications
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