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Alvelestat tosylate

Names

[ CAS No. ]:
1240425-05-1

[ Name ]:
Alvelestat tosylate

[Synonym ]:
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

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C32H30F3N5O7S2

[ Molecular Weight ]:
717.73500

[ Exact Mass ]:
717.15400

[ PSA ]:
187.08000

[ LogP ]:
7.08790

Related Compounds