LY 3000328 is a highly selective and potent Cathepsin S inhibitor with IC50 of 7.7±5.85 nM and 1.67±1.17 nM for hCat S and mCat S respectively, can be used in treatment for abdominal aortic aneurysm.
LY3000328 is a non-covalent, non-peptidic and selective Cathepsin S inhibitor with IC50 values of 7.7nM and 1.67nM for hCathepsin S and mCathepsin S, respectively. Oral administration of LY3000328, BID, for 28 days reduced aortic diameter induced by CaCl2 by 58%, 83% and 87% at dose of 1, 3 and 10mg/kg[1]. LY3000328 showed cleared quickly from plasma. A Phase 1 study of LY-3000328 has been completed.[2].
作用机制
LY3000328 binds to the S2 and S3 subsites of Cathepsin S without interacting with the active site Cys25.[1]
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