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A mast cell tryptase inhibitor
APC 366 is a mast cell tryptase inhibitor (Ki = 7.1 μM for human recombinant enzyme). It reduces maximum contractile response to histamine in isolated bronchial tissue from ovalbumin-sensitized guinea pigs when used at a concentration of 1 μM. Aerosolized APC 366 (5 mg in 1 ml of water) reduces airway resistance and increases dynamic lung compliance in A. suum antigen-challenged pigs. It also reduces collagen content and expression of protease-activated receptor 2 (PAR-2) and α-smooth muscle actin (α-SMA) in rat liver in a model of bile duct ligation-induced liver fibrosis.
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