| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
CRA-2059 TFA is a highly specific and selective tryptase inhibitor. It targets recombinant human tryptase-beta (rHTbeta) with an exceptionally high binding affinity. Tryptase is a trypsin-like serine protease and a major protein component in human mast cell secretory granules. CRA-2059 is highly selective for tryptase over other serine proteases.
|
|---|---|
| ln Vitro |
Tryptase is a serine protease that resembles trypsin and is the main protein found in human mast cell secretory granules. Research on inflammatory bowel illness may benefit from the usage of CRA-2059 [1].
CRA-2059 TFA is a highly specific and selective tryptase inhibitor with a Ki of 620 pM (0.62 nM) for recombinant human tryptase-beta (rHTbeta). It demonstrates excellent potency in enzymatic assays, effectively blocking the proteolytic activity of tryptase at low picomolar concentrations. Tryptase is a major protein in human mast cell secretory granules. |
| ln Vivo |
CRA-2059 has shown potential for inflammatory bowel disease (IBD) research. A related tryptase inhibitor (APC 2059) has been evaluated in an open-label pilot study for the treatment of mildly to moderately active ulcerative colitis. This suggests potential for anti-inflammatory applications, though detailed in vivo efficacy data for CRA-2059 TFA in animal models is limited.
|
| Enzyme Assay |
For in vitro enzyme inhibition assays (non-cell-based), recombinant human tryptase-beta (rHTbeta) is incubated with a fluorogenic tryptase substrate (e.g., tosyl-Gly-Pro-Lys-4-amidobenzotriazole or similar) in assay buffer (0.1 M Tris-HCl, pH 8.0, 0.1 M NaCl, 0.1 mg/mL heparin). Varying concentrations of CRA-2059 TFA (0-10 nM) are pre-incubated with the enzyme for 10 minutes at 37degC. The substrate is then added, and fluorescence (excitation 360 nm, emission 460 nm) is measured kinetically for 30 minutes. Ki is calculated from the dose-response curve.
|
| Cell Assay |
CRA-2059 TFA is typically not used in direct cellular assays as it targets the secreted protease tryptase rather than intracellular targets. For functional assays, mast cells (e.g., LAD2 or HMC-1) can be stimulated to degranulate (e.g., with calcium ionophore or IgE cross-linking) in the presence or absence of CRA-2059 TFA (0-100 nM). The inhibition of tryptase activity in the supernatant is measured by adding a fluorogenic substrate to the collected medium.
|
| Animal Protocol |
For animal studies, CRA-2059 TFA may be administered to rodent models of inflammatory bowel disease (e.g., dextran sulfate sodium (DSS)-induced colitis in mice) or other mast cell-mediated inflammatory conditions. Dosing is typically by intraperitoneal injection (e.g., 1-10 mg/kg once or twice daily). Colitis severity is assessed by disease activity index (DAI), colon length, and histopathological scoring. Detailed protocols are not standardized.
|
| ADME/Pharmacokinetics |
CRA-2059 TFA has a molecular weight of 864.83 Da. The TFA salt form enhances water solubility compared to the free base. As a peptide, CRA-2059 is susceptible to proteolytic degradation in vivo. It is stored as a lyophilized powder at -20degC. For in vivo administration, it can be formulated in saline or PBS (with 0.1% BSA to prevent adsorption). Preliminary pharmacokinetic data is limited.
|
| Toxicity/Toxicokinetics |
CRA-2059 TFA is a research-grade compound not for human use. At picomolar to nanomolar concentrations in enzyme assays, it shows no non-specific effects. Standard safety studies (cytotoxicity, off-target protease panel) would be required for further development. Based on the mechanism of tryptase inhibition, no significant toxicity is expected at therapeutic doses in research animals.
|
| References | |
| Additional Infomation |
CRA-2059 TFA (CAS: not specified for TFA salt; sequence-based) is a synthetic peptide inhibitor of tryptase. It is a research tool for studying the role of tryptase in mast cell biology, allergic inflammation, and gastrointestinal disorders such as ulcerative colitis and Crohn's disease. Purity is typically ≥98% by HPLC. It is not approved for clinical use.
|
| Molecular Formula |
C36H47F3N12O10
|
|---|---|
| Molecular Weight |
864.83
|
| Related CAS # |
CRA-2059;256649-36-2;CRA-2059 hydrochloride
|
| Appearance |
White to light yellow solid powder
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO :~100 mg/mL (~115.63 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.89 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.89 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.89 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1563 mL | 5.7815 mL | 11.5630 mL | |
| 5 mM | 0.2313 mL | 1.1563 mL | 2.3126 mL | |
| 10 mM | 0.1156 mL | 0.5781 mL | 1.1563 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
