An elective, selective inhibitor of the mast cell tryptase, which inhibits tryptase-induced histamine release from human tonsil and lung cells. It can reduce airway inflammation and block postchallenge airway hyperresponsiveness in vivo.
CAT No: R0892
CAS No:158921-85-8
Synonyms/Alias:N-(1-Hydroxy-2-naphthoyl)-L-arginyl-L-prolinamide
In sheep naturally sensitized to Ascaris suum , the novel selective inhibitor of tryptase APC 366 [N-(1-hydroxy-2-naphthoyl)-L-arginyl-L-prolinamide] attenuates the EAR, the LAR, acquired BHR, and the accompanying influx of inflammatory leukocytes on aerosol challenge with an antigenic extract. It has been shown that APC 366 inactivates tryptase in a time-dependent and irreversible manner involving slow isomerization of the hydroxynaphthyl group of APC 366 followed by nucleophilic attack of a tryptase amino acid side chain to result in the formation of a nonhydrolyzable covalent adduct between inhibitor and enzyme.
Inhibition of mast cell tryptase by inhaled APC 366 attenuates allergen-induced late-phase airway obstruction in asthma
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