1240425-05-1
Chemical Structure
Alvelestat tosylate
Synonym(s): AZD9668 tosylate
- CAS No.: 1240425-05-1
- Formula:C32H30F3N5O7S2
- Molecular Weight:717.74
IUPAC Name: 6-methyl-5-(1-methyl-1H-pyrazol-5-yl)-N-((5-(methylsulfonyl)pyridin-2-yl)methyl)-2-oxo-1-(3-(trifluoromethyl)phenyl)-1,2-dihydropyridine-3-carboxamide 4-methylbenzenesulfonate
InChIKey: YLZZBCWZQPXIHL-UHFFFAOYSA-N
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.O=S(C5=CC=C(C)C=C5)(O)=O
Biological Activity: Alvelestat tosylate (AZD9668 tosylate) is an orally active, selective inhibitor of neutrophil elastase. Alvelestat tosylate reduces elastase activity, myeloperoxidase release, neutrophil recruitment and activation, and calcium phosphate precipitation; promotes smooth muscle cell colonization and collagen deposition; and inhibits the formation of neutrophil extracellular traps (NETs) as well as NET-derived neutrophil elastase activity. Alvelestat tosylate restores endothelial dysfunction, regulates antioxidant factors, improves the expression of endothelial tight junctions, reduces vascular leakage, and accelerates wound healing. Alvelestat tosylate prevents pulmonary hemorrhage, matrix protein degradation, airspace enlargement, and small airway wall remodeling; and alleviates cigarette-induced inflammatory responses. Alvelestat tosylate inhibits the growth of abdominal aortic aneurysms exacerbated by Porphyromonas gingivalis. Alvelestat tosylate can be used in research related to chronic obstructive pulmonary disease, abdominal aortic aneurysm, radiation-induced skin injury, and bronchiectasis[1][2][3][4].
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Alvelestat tosylate | Alvelestat tosylate (AZD9668 tosylate) is an orally active, selective inhibitor of neutrophil elastase. Alvelestat tosylate reduces elastase activity, myeloperoxidase release, neutrophil recruitment and activation, and calcium phosphate precipitation; promotes smooth muscle cell colonization and collagen deposition; and inhibits the formation of neutrophil extracellular traps (NETs) as well as NET-derived neutrophil elastase activity. Alvelestat tosylate restores endothelial dysfunction, regulates antioxidant factors, improves the expression of endothelial tight junctions, reduces vascular leakage, and accelerates wound healing. Alvelestat tosylate prevents pulmonary hemorrhage, matrix protein degradation, airspace enlargement, and small airway wall remodeling; and alleviates cigarette-induced inflammatory responses. Alvelestat tosylate inhibits the growth of abdominal aortic aneurysms exacerbated by Porphyromonas gingivalis. Alvelestat tosylate can be used in research related to chronic obstructive pulmonary disease, abdominal aortic aneurysm, radiation-induced skin injury, and bronchiectasis. | |||||||||||||||||||||
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- [1]. Vogelmeier C, et al. A randomised, placebo-controlled, dose-finding study of AZD9668, an oral inhibitor of neutrophil elastase, in patients with chronic obstructive pulmonary disease treated with tiotropium. COPD. 2012 Apr;9(2):111-20. [Content Brief]
- [2]. Delbosc S, et al. Elastase inhibitor AZD9668 treatment prevented progression of experimental abdominal aortic aneurysms. Journal of vascular surgery. 2016 Feb;63(2):486-92.e1. [Content Brief]
- [3]. Park JH, et al. AZD 9668, a neutrophil elastase inhibitor, promotes wound healing in the irradiated skin by inhibiting NET-derived vascular dysfunction. International immunopharmacology. 2025 Jun 26;159:114860. [Content Brief]
- [4]. Stevens T, et al. AZD9668: pharmacological characterization of a novel oral inhibitor of neutrophil elastase. The Journal of pharmacology and experimental therapeutics. 2011 Oct;339(1):313-20. [Content Brief]
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