| 名称 | LY 3000328 |
| 描述 | 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. |
| 体外活性 | 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] |
| 体内活性 | 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] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 48 mg/mL (99.06 mM)
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| 关键字 | LY 3000328 | Cathepsin | Inhibitor | inhibit | LY3000328 | LY-3000328 |
| 相关产品 | Papain | 2-Aminoethanethiol | (S)-(+)-Ibuprofen | PMSF | KGP94 | N-Ethylmaleimide | Z-Lys-OH | Leupeptin Hemisulfate | 2-Cyanopyrimidine | Esomeprazole | Aloxistatin | E-64 |
| 相关库 | 经典已知活性库 | ReFRAME 相关化合物库 | 蛋白酶抑制剂库 | 抑制剂库 | 已知活性化合物库 |
United States
