Alvelestat tosylate

Modify Date: 2024-01-05 19:59:14

Alvelestat tosylate Structure
Alvelestat tosylate structure
Common Name Alvelestat tosylate
CAS Number 1240425-05-1 Molecular Weight 717.73500
Density N/A Boiling Point N/A
Molecular Formula C32H30F3N5O7S2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Alvelestat tosylate


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].

 Names

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
Synonym More Synonyms

 Alvelestat 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
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

 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
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