CRA-2059 TFA
Based on 1 Customer Validation
CRA-2059 is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ).
For research use only. We do not sell to patients.
- Purity: 99.88%
- Formula: C36H47F3N12O10
- Molecular Weight:864.83
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Bioactive Compound Library Max
HY-L181
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Bioactive Compound Library
HY-L001
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Immunology/Inflammation Compound Library
HY-L007
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Metabolism/Protease Compound Library
HY-L012
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Coagulation and Anti-coagulation Compound Library
HY-L136
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Heterocyclic Compound Library
HY-L138
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Protease Inhibitor Library
HY-L147
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Highly Selective Inhibitors Library
HY-L158
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Serine/Threonine Kinase Inhibitor Library
HY-L164
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MCE Bioactive Compound Library
HY-L001V
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Protein Kinase Compound Library
HY-L196
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
Tryptase is a trypsin-like serine protease found as a major protein component in human mast cell secretory granules. CRA-2059 has the potential for inflammatory bowel disease research[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Solid
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Molecular Weight 864.83
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Formula C36H47F3N12O10
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Color White to light yellow
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SMILES
NC(NC1=CC=C(CNC(N2CCN(C(O[C@@H]3COC4[C@H](OC(N5CCN(C(NCC6=CC=C(NC(N)=N)C=C6)=O)CC5)=O)COC34)=O)CC2)=O)C=C1)=N.FC(F)(F)C(O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (115.63 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.
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 (2.89 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 (2.89 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. * 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.
Purity & Documentation
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Data Sheet (271 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]. Tremaine WJ, et al. Treatment of mildly to moderately active ulcerative colitis with a tryptase inhibitor (APC 2059): an open-label pilot study. Aliment Pharmacol Ther. 2002;16(3):407-413. [Content Brief]
[2]. Selwood T, et al. Potent bivalent inhibition of human tryptase-beta by a synthetic inhibitor. Biol Chem. 2003;384(12):1605-1611. [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 | 1.1563 mL | 5.7815 mL | 11.5630 mL | 28.9074 mL |
| 5 mM | 0.2313 mL | 1.1563 mL | 2.3126 mL | 5.7815 mL | |
| 10 mM | 0.1156 mL | 0.5781 mL | 1.1563 mL | 2.8907 mL | |
| 15 mM | 0.0771 mL | 0.3854 mL | 0.7709 mL | 1.9272 mL | |
| 20 mM | 0.0578 mL | 0.2891 mL | 0.5781 mL | 1.4454 mL | |
| 25 mM | 0.0463 mL | 0.2313 mL | 0.4625 mL | 1.1563 mL | |
| 30 mM | 0.0385 mL | 0.1927 mL | 0.3854 mL | 0.9636 mL | |
| 40 mM | 0.0289 mL | 0.1445 mL | 0.2891 mL | 0.7227 mL | |
| 50 mM | 0.0231 mL | 0.1156 mL | 0.2313 mL | 0.5781 mL | |
| 60 mM | 0.0193 mL | 0.0964 mL | 0.1927 mL | 0.4818 mL | |
| 80 mM | 0.0145 mL | 0.0723 mL | 0.1445 mL | 0.3613 mL | |
| 100 mM | 0.0116 mL | 0.0578 mL | 0.1156 mL | 0.2891 mL |
CRA-2059 TFA Related Classifications
HY-19303B Related Classifications
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