LY3000328 is a potent cathepsin S inhibitor (IC50 = 7.7 nM for the human enzyme). It is selective for cathepsin S over cathepsin L, K, B, and V (IC50s = >10,000, >10,000, 4,390, and 21,500 nM, respectively). LY3000328 (1-30 mg/kg) reduces aortic diameter in a mouse model of calcium chloride-induced abdominal aortic aneurysm.
LY 3000328 is a cathepsin S inhibitor for treatment of abdominal aortic aneurysm. Further provides methods for treating plaque instability, atherosclerosis, or autoimmune disorders such as rheumatoid arthritis, psoriasis, and lupus comprising administering a therapeutically effective amount of a disclosed compound.
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