INVA8001 (ASB17061) is a highly selective and orally active chymase inhibitor with IC 50 values for human chymase and mouse mast cell proteinase 4 ( mMCP-4 ) of 0.02 and 0.03 μM, respectively. INVA8001 exhibits IC 50 values for bovine α-chymotrypsin and human cathesin G of 3.4 and 32.1 μM, respectively, and it shows over 1000-fold selectivity for other related serine proteases. INVA8001 inhibits mast cells in a mouse primary sclerosing cholangitis (PSC) model, improves bile duct pathology, and alleviates bile stasis, demonstrating anti-inflammatory and anti-fibrotic effects.
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