Alvelestat
Based on 11 publication(s) in Google Scholar
Alvelestat (AZD9668) is an orally bioavailable, affinity and selective inhibitor of neutrophil elastase (NE) with a pIC50 value of 7.9 nM, a Ki value of 9.4 nM and a Kd value of 9.5 nM.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.87%
- CAS No.: 848141-11-7
- Formule: C25H22F3N5O4S
- Masse moléculaire:545.53
-
Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
-
Immunology/Inflammation Compound Library
HY-L007
-
Metabolism/Protease Compound Library
HY-L012
-
Anti-diabetic Compound Library
HY-L040
-
Pyroptosis Compound Library
HY-L059
-
Orally Active Compound Library
HY-L061
-
Targeted Diversity Library
HY-L099
-
Rare Diseases Drug Library
HY-L102
-
Human Metabolite Library
HY-L123
-
Protease Inhibitor Library
HY-L147
-
Highly Selective Inhibitors Library
HY-L158
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
Publications Citing Use of MedChemExpress (MCE) Alvelestat
More- Cancer Cell. 2021 Mar 8;39(3):423-437.e7. [Abstract]
- Cell Death Dis. 2025 Apr 8;16(1):264. [Abstract]
- J Immunother Cancer. 2025 Feb 26;13(2):e010813. [Abstract]
- Neural Regen Res. 2023 Oct;18(10):2252-2259. [Abstract]
- NPJ Regen Med. 2020 Oct 30;5(1):19. [Abstract]
- Int J Mol Sci. 2024 Dec 27;26(1):143. [Abstract]
- Int Immunopharmacol. 2024 Nov 5;143(Pt 3):113534. [Abstract]
- FEBS Open Bio. 2018 Mar 25;8(5):751-763. [Abstract]
- bioRxiv. 2025 February 28.
- bioRxiv. 2023 Nov 13.
- Biomed Pharmacother. 2021 Feb:134:111152. [Abstract]
Activité biologique
pIC: 7.9 nM; Ki: 9.4 nM; Kd: 9.5 nM (neutrophil elastas)[1]
Alvelestat (20 μg/mL; 16 hours; HBE and A549 cells) treatment decreases cells death and decreases the levels of IL-1β, IL-6, and TNF-α in vitro[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Human bronchial epithelial cells (HBE) and human alveolar epithelial cells (A549)
-
Concentration:20 μg/mL
-
Incubation Time:16 hours
-
Result:Decreased cytotoxicity and inflammatory responses.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Female BALB/cJBomTac mice exposed to smoke cigarette smoke[1]
-
Dosage:1 mg/kg , 3 mg/kg , 6 mg/kg , 10 mg/kg
-
Administration:Oral administration; twice daily; for 4 days
-
Result:Reduced the inflammatory response to cigarette smoke as indicated by a reduction in BAL neutrophils and interleukin-1β.
Chemical Information
-
CAS No. 848141-11-7
-
Appearance Solid
-
Masse moléculaire 545.53
-
Formule C25H22F3N5O4S
-
Color White to light yellow
-
SMILES
O=C(C1=CC(C2=CC=NN2C)=C(C)N(C3=CC=CC(C(F)(F)F)=C3)C1=O)NCC4=NC=C(S(=O)(C)=O)C=C4
-
Synonyms
AZD9668
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (11)
-
Journal Impact Factor
-
Most Recent
-
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 -
Cell Death Dis
Downregulation of tropomyosin 2 promotes the progression of lung adenocarcinoma by regulating neutrophil infiltration through neutrophil elastase. [Abstract]2025 Apr 8;16(1):264. PMID: 40199876 -
J Immunother Cancer
Neutrophil extracellular traps impede cancer metastatic seeding via protease-activated receptor 2-mediated downregulation of phagocytic checkpoint CD24. [Abstract]2025 Feb 26;13(2):e010813. PMID: 40010762 -
Neural Regen Res
2023 Oct;18(10):2252-2259. PMID: 37056145 -
NPJ Regen Med
2020 Oct 30;5(1):19. PMID: 33298919 -
Int J Mol Sci
Neutrophil Extracellular Trap Formation Model Induced by Monosodium Urate and Phorbol Myristate Acetate: Involvement in MAPK Signaling Pathways. [Abstract]2024 Dec 27;26(1):143. PMID: 39796001 -
Int Immunopharmacol
HSYA ameliorates venous thromboembolism by depleting the formation of TLR4/NF-κB pathway-dependent neutrophil extracellular traps. [Abstract]2024 Nov 5;143(Pt 3):113534. PMID: 39504860 -
FEBS Open Bio
Identification of small-molecule elastase inhibitors as antagonists of IL-36 cytokine activation. [Abstract]2018 Mar 25;8(5):751-763. PMID: 29744290 -
-
-
Biomed Pharmacother
Neutrophil elastase inhibitor (MPH-966) improves intestinal mucosal damage and gut microbiota in a mouse model of 5-fluorouracil-induced intestinal mucositis. [Abstract]2021 Feb:134:111152. PMID: 33373916
Solvant et solubilité
DMSO : ≥ 33 mg/mL (60.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (4.58 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 (4.58 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Pureté et documentation
-
Fiche technique (275 KB)
-
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)
-
Instruction de manipulation (2659 KB)
Références
[1]. Stevens T, et al. AZD9668: pharmacological characterization of a novel oral inhibitor of neutrophil elastase. J Pharmacol Exp Ther. 2011 Oct;339(1):313-20. [Content Brief]
[2]. Li H, et al. Neutrophil extracellular traps contribute to the pathogenesis of acid-aspiration-induced ALI/ARDS. Oncotarget. 2017 Nov 28;9(2):1772-1784. [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, 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8331 mL | 9.1654 mL | 18.3308 mL | 45.8270 mL |
| 5 mM | 0.3666 mL | 1.8331 mL | 3.6662 mL | 9.1654 mL | |
| 10 mM | 0.1833 mL | 0.9165 mL | 1.8331 mL | 4.5827 mL | |
| 15 mM | 0.1222 mL | 0.6110 mL | 1.2221 mL | 3.0551 mL | |
| 20 mM | 0.0917 mL | 0.4583 mL | 0.9165 mL | 2.2913 mL | |
| 25 mM | 0.0733 mL | 0.3666 mL | 0.7332 mL | 1.8331 mL | |
| 30 mM | 0.0611 mL | 0.3055 mL | 0.6110 mL | 1.5276 mL | |
| 40 mM | 0.0458 mL | 0.2291 mL | 0.4583 mL | 1.1457 mL | |
| 50 mM | 0.0367 mL | 0.1833 mL | 0.3666 mL | 0.9165 mL | |
| 60 mM | 0.0306 mL | 0.1528 mL | 0.3055 mL | 0.7638 mL |
Alvelestat Related Classifications
HY-15651 Related Classifications
Powered by Bioz