INVA8001 is a highly selective and orally active chymase inhibitor, demonstrating significant potency with IC50 values of 0.02 μM for human chymase and 0.03 μM for mouse mast cell proteinase 4 (mMCP-4). This compound exhibits remarkable selectivity over related serine proteases, with IC50 values of 3.4 μM for bovine α-chymotrypsin and 32.1 μM for human cathepsin G, showcasing over 1000-fold selectivity. INVA8001 has been shown to inhibit mast cell activity in a mouse model of primary sclerosing cholangitis (PSC), leading to improved bile duct pathology and reduced bile stasis, thus highlighting its potential anti-inflammatory and anti-fibrotic applications in research.
INVA8001 is a highly selective and orally active chymase inhibitor, demonstrating significant potency with IC50 values of 0.02 μM for human chymase and 0.03 μM for mouse mast cell proteinase 4 (mMCP-4). This compound exhibits remarkable selectivity over related serine proteases, with IC50 values of 3.4 μM for bovine α-chymotrypsin and 32.1 μM for human cathepsin G, showcasing over 1000-fold selectivity. INVA8001 has been shown to inhibit mast cell activity in a mouse model of primary sclerosing cholangitis (PSC), leading to improved bile duct pathology and reduced bile stasis, thus highlighting its potential anti-inflammatory and anti-fibrotic applications in research.
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