TY-51469

TY-51469 is a potent, highly selective, small-molecule chymase inhibitor originally developed by Toa Eiyo. It inhibits chymase with IC50 values of 0.4 nM for simian chymase and 7.0 nM for human chymase, demonstrating high selectivity over other serine proteases such as bovine chymotrypsin and human cathepsin G. Chymase is a mast cell-specific serine protease that plays a key role in angiotensin II generation, TGF-beta activation, and matrix metalloproteinase (MMP) activation, contributing to tissue remodeling, inflammation, and fibrosis. Preclinical studies have demonstrated that TY-51469 ameliorates gut permeability and inflammation in models of inflammatory bowel disease (IBD) and colitis, reduces silica-induced pulmonary fibrosis, prevents diabetic kidney disease (DKD) and pancreatic islet disorganization, and protects against deep vein thrombosis (DVT) and cardiac remodeling.

Other names

2-(4-((5-fluoro-3-methylbenzo-[b]thiophene)-2-sulfonamido)-3-(methylsulfonyl)phenyl)thiazole-4-carboxylic acid2-[4-(5-fluoro-3-methylbenzo[b]thiophen-2-yl)sulfonamido-3-methanesulfonylphenyl]thiazole-4-carboxylic acid