Brensocatib
Based on 7 publication(s) in Google Scholar
Brensocatib (AZD7986) is an oral dipeptidyl peptidase 1 (DPP1) inhibitor with pIC50s of 6.85, 7.6, 7.7, 7.8, and 7.8 in human, mouse, rat, dog and rabbit, respectively.
For research use only. We do not sell to patients.
- Purity: 99.88%
- CAS No.: 1802148-05-5
- Formula: C23H24N4O4
- Molecular Weight:420.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Brensocatib
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Customer Validation & Images
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In Vivo Efficacy Study
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Histological Imaging/Staining
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In Vivo Efficacy Study
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ELISA
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Cell Imaging/Staining
Biological Activity
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DPP-1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| L02 | IC50 |
>100 μM
Compound: AZD7986
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Cytotoxicity against human L02 cells assessed as cell viability incubated for 48 hrs by CCK-8 assay
Cytotoxicity against human L02 cells assessed as cell viability incubated for 48 hrs by CCK-8 assay
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[PMID: 34374541] |
Results from cell assay show that Brensocatib (AZD7986) is a Dipeptidyl peptidase 1 (DPP1) inhibitor with pIC50s of 6.85, 7.6, 7.7, 7.8, and 7.8 in human, mouse, rat, dog and rabbit, respectively. Brensocatib is stable in the propionaldehyde reactivity assay, with a half-life over 50 h. After differentiation in the presence of Brensocatib (38 pM to 10 μM), concentration-dependent decreases in cell lysate enzyme activity are observed for DPP1, as well as for all of the three NSPs, NE, Pr3, and CatG. Brensocatib inhibits activation of all three NSPs in a concentration dependent manner, with pIC50 values of around 7 for all three NSPs. The reduction of the activities is almost complete, with NE, Pr3, and CatG activities reduced to 4 to 10% of control at 10 μM Brensocatib[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1802148-05-5
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Appearance Solid
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Molecular Weight 420.46
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Formula C23H24N4O4
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Color White to light yellow
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SMILES
O=C([C@H]1OCCCNC1)N[C@H](C#N)CC2=CC=C(C3=CC=C(OC(N4C)=O)C4=C3)C=C2
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Synonyms
AZD7986; INS 1007
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Cathepsin C promotes breast cancer lung metastasis by modulating neutrophil infiltration and neutrophil extracellular trap formation. [Abstract]2021 Mar 8;39(3):423-437.e7. PMID: 33450198
Brensocatib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Mar 8;39(3):423-437.e7. [Abstract]
Brensocatib (AZD7986) (5 mg/kg; p.o.; twice daily) effectively restored body weight and extended overall survival of mice after orthotopic injection of 4T1 cells.
Brensocatib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Mar 8;39(3):423-437.e7. [Abstract]
Brensocatib (AZD7986) (5 mg/kg; p.o.; twice daily). NET staining and quantitation in lungs of mice after orthotopic injection of 4T1.
Brensocatib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Mar 8;39(3):423-437.e7. [Abstract]
Brensocatib (AZD7986) (5 mg/kg; p.o.; twice daily). Lung-metastatic nodules at week 7 of mice after orthotopic injection of AT3.
Brensocatib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Mar 8;39(3):423-437.e7. [Abstract]
Brensocatib (AZD7986) (5 mg/kg; p.o.; twice daily) suppressed circulating IL-1b levels in the mice after orthotopic injection of AT3.
Brensocatib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Mar 8;39(3):423-437.e7. [Abstract]
NETosis of murine neutrophils was pre-treated with Brensocatib (AZD7986) (10 μM).
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Theranostics
2024 May 13;14(8):3029-3042. PMID: 38855187 -
Redox Biol
Cathepsin C from extracellular histone-induced M1 alveolar macrophages promotes NETosis during lung ischemia-reperfusion injury. [Abstract]2024 Aug:74:103231. PMID: 38861835 -
Biochem Pharmacol
Structure-based design and in vivo anti-arthritic activity evaluation of a potent dipeptidyl cyclopropyl nitrile inhibitor of cathepsin C. [Abstract]2019 Jun;164:349-367. PMID: 30978322 -
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Solvent & Solubility
DMSO : 100 mg/mL (237.83 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (5.95 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.
Protocol
Cellular potency is studied using the DPP1-expressing monocytic U937 cell line. Briefly, cells grown in RPMI are plated on 384-well polypropylene v-bottom plates at a density of 5×105 cells/mL per well. Added to this is 10 μL of Brensocatib at 37°C for 60 min, followed by 350 μM Gly-Phe-AFC. The well fluorescence is read using a multilabel plate reader. Data are analyzed to calculate pIC50 values[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats are used for the in vivo study. Naive rats are dosed orally twice daily with Brensocatib at 0.2, 2, and 20 mg/kg/day for 8 days. At termination, bone marrow is taken by femural aspiration for neutrophil serine proteases (NSPs) activity analysis using commercial synthetic peptide substrates[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (643 KB)
- English - EN (643 KB)
- Français - FR (643 KB)
- Deutsch - DE (643 KB)
- Norwegian - NO (643 KB)
- Español - ES (643 KB)
- Swedish - SV (643 KB)
- Italian - IT (643 KB)
- Portuguese - PT (643 KB)
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Handling Instructions (2659 KB)
References
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.3783 mL | 11.8917 mL | 23.7835 mL | 59.4587 mL |
| 5 mM | 0.4757 mL | 2.3783 mL | 4.7567 mL | 11.8917 mL | |
| 10 mM | 0.2378 mL | 1.1892 mL | 2.3783 mL | 5.9459 mL | |
| 15 mM | 0.1586 mL | 0.7928 mL | 1.5856 mL | 3.9639 mL | |
| 20 mM | 0.1189 mL | 0.5946 mL | 1.1892 mL | 2.9729 mL | |
| 25 mM | 0.0951 mL | 0.4757 mL | 0.9513 mL | 2.3783 mL | |
| 30 mM | 0.0793 mL | 0.3964 mL | 0.7928 mL | 1.9820 mL | |
| 40 mM | 0.0595 mL | 0.2973 mL | 0.5946 mL | 1.4865 mL | |
| 50 mM | 0.0476 mL | 0.2378 mL | 0.4757 mL | 1.1892 mL | |
| 60 mM | 0.0396 mL | 0.1982 mL | 0.3964 mL | 0.9910 mL | |
| 80 mM | 0.0297 mL | 0.1486 mL | 0.2973 mL | 0.7432 mL | |
| 100 mM | 0.0238 mL | 0.1189 mL | 0.2378 mL | 0.5946 mL |
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