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LY 3000328 (Cathepsin S inhibitor) is a selective inhibitor of cathepsin S with IC50 values of 7.7 and 1.67 nM for human and mouse cathepsin S, respectively. LY 3000328 (Cathepsin S inhibitor) may slow or prevent abdominal aortic aneurysm (AAA) expansion and/or reduce the risk of AAA rupture by inhibiting cathepsin S-mediated degradation of extracellular matrix proteins, elastin and collagen.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $97 | In Stock | |
2 mg | $139 | In Stock | |
5 mg | $221 | In Stock | |
10 mg | $292 | In Stock | |
25 mg | $513 | In Stock | |
50 mg | $746 | In Stock | |
100 mg | $1,050 | In Stock | |
1 mL x 10 mM (in DMSO) | $231 | In Stock |
Description | LY 3000328 (Cathepsin S inhibitor) is a selective inhibitor of cathepsin S with IC50 values of 7.7 and 1.67 nM for human and mouse cathepsin S, respectively. LY 3000328 (Cathepsin S inhibitor) may slow or prevent abdominal aortic aneurysm (AAA) expansion and/or reduce the risk of AAA rupture by inhibiting cathepsin S-mediated degradation of extracellular matrix proteins, elastin and collagen. |
Targets&IC50 | Cathepsin S (mouse):1.67 nM, Cathepsin S (human):7.7 nM |
In vitro | METHODS: The activity of LY 3000328 (Cathepsin S inhibitor) was evaluated in hCat S and mCat S enzyme inhibition assays. RESULTS The IC50 values of LY 3000328 (Cathepsin S inhibitor) for inhibiting human and mouse Cat S were 7.7±5.85 and 1.67±1.17 nM, respectively. [1] |
In vivo | METHODS: The efficacy of LY 3000328 (Cathepsin S inhibitor)(1, 3, 10, 30 mg/kg, oral, 28 days) in BID mice was studied. RESULTS When the lowest dose of LY 3000328 (Cathepsin S inhibitor) was 1 mg/kg, the aortic diameter decreased by 58%, 83% at 3 mg/kg, and 87% at 10 mg/kg; the exposure (AUC) of LY 3000328 (Cathepsin S inhibitor) increased in a dose-dependent manner, indicating good drug disposition performance. [1] |
Alias | Cathepsin S inhibitor |
Molecular Weight | 484.52 |
Formula | C25H29FN4O5 |
Cas No. | 1373215-15-6 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 48 mg/mL (99.06 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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