| Name | LY 3000328 |
| 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. |
| 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] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.13 mM), Sonication is recommended.
DMSO : 62.5 mg/mL (128.99 mM), Sonication is recommended.
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| Keywords | LY-3000328 | LY3000328 | LY 3000328 | Inhibitor | inhibit | CysteineProtease | Cysteine Protease | Cathepsin S | Cathepsin |
| Inhibitors Related | Papain | 2-Aminoethanethiol | (S)-(+)-Ibuprofen | Asperphenamate | PMSF | JNJ-10311795 | N-Ethylmaleimide | Z-Lys-OH | Esomeprazole | 2-Cyanopyrimidine | Aloxistatin | 4-Methylesculetin |
| Related Compound Libraries | Bioactive Compound Library | ReFRAME Related Library | Protease Inhibitor Library | Drug Repurposing Compound Library | Inhibitor Library | Clinical Compound Library | Bioactive Compounds Library Max | Fluorochemical Library |
United States
