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Beschreibung

A cell-permeable, competitive Acidic Mammalian Chitinase (AMCase) Inhibitor (IC50 = 0.92 µ,M and Ki = 0.42 µ,M for hAMCase, and IC50= 2.2 µ,M for mAMCase, in vitro) that demonstrates 20-fold selectivity for hAMCase over hCHIT1. It is shown to decrease chitinase enzymatic activity (5 mg/kg, i.p.) in the lungs of control PBS- and OVA-challenged mice. Furthermore, it attenuates lung chitinase activity, reduces eosinophil influx, and improves ventilatory function, in vivo, in a murine model of allergic inflammation. It also causes neutrophilia in the lungs of OVA-challenged mice.