INVA8001 is a highly selective and orally active chymase inhibitor, with IC50 values of 0.02 µM for human chymase and 0.03 µM for mouse mast cell protease 4 (mMCP-4). It exhibits IC50 values of 3.4 µM for bovine alpha-chymotrypsin and 32.1 µM for human cathepsin G, demonstrating over 1000-fold selectivity against other related serine proteases. In a mouse model of primary sclerosing cholangitis (PSC), INVA8001 inhibits mast cell activity, improves biliary pathology, alleviates cholestasis, and displays anti-inflammatory and anti-fibrotic properties.
Molekulargewicht:
620.1
CAS Nummer:
[1312993-34-2]
Formel:
C29H38ClN5O8
Target-Kategorie:
Proteasome
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