1240425-05-1

1240425-05-1 structure

Name: Alvelestat tosylate
Chemical Name: 4-methylbenzenesulfonic acid,6-methyl-5-(2-methylpyrazol-3-yl)-N-[(5-methylsulfonylpyridin-2-yl)methyl]-2-oxo-1-[3-(trifluoromethyl)phenyl]pyridine-3-carboxamide
CAS Number: 1240425-05-1
Molecular Formula: C₃₂H₃₀F₃N₅O₇S₂
Molecular Weight: 717.73500
Create Date: 2016-10-12 07:31:38
Modify Date: 2024-01-05 19:59:14
Alvelestat (tosylate) 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[1].

Name	4-methylbenzenesulfonic acid,6-methyl-5-(2-methylpyrazol-3-yl)-N-[(5-methylsulfonylpyridin-2-yl)methyl]-2-oxo-1-[3-(trifluoromethyl)phenyl]pyridine-3-carboxamide
Synonyms	UNII-E1B3T25UM9 Alvelestat tosilate Alvelestat tosylate 3-Pyridinecarboxamide,1,2-dihydro-6-methyl-5-(1-methyl-1H-pyrazol-5-yl)-N-((5-(methylsulfonyl)-2-pyridinyl)methyl)-2-oxo-1-(3-(trifluoromethyl)phenyl)-,4-methylbenzenesulfonate (1:1) AZD-9668 tosylate

Description	Alvelestat (tosylate) 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[1].
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Elastase Research Areas >> Inflammation/Immunology
Target	pIC: 7.9 nM; Ki: 9.4 nM; Kd: 9.5 nM (neutrophil elastas)[1]
In Vitro	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].
References	[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. [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.