货号:A473978 同义名: Z-FL-COCHO;Compound 5
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.
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产品名称 | Cysteine Protease ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Z-FA-FMK | ✔ | 99%+ | |||||||||||||||||
Leupeptin hemisulfate | ✔ | 97% | |||||||||||||||||
PMSF | ✔ | 95% | |||||||||||||||||
PD 151746 |
+
μ-Calpain, IC50: 260 nM m-calpain, IC50: 5.33 μM |
98% | |||||||||||||||||
Odanacatib |
++++
Cathepsin K (human), IC50: 0.2 nM Cathepsin K (rabbit), IC50: 1 nM |
99%+ | |||||||||||||||||
E-64 |
+++
Cysteine protease, IC50: 9 nM |
99%+ | |||||||||||||||||
E 64c | ✔ | 95% | |||||||||||||||||
E-64d | ✔ | 99%+ | |||||||||||||||||
MG-101 | ✔ | 98%+ | |||||||||||||||||
Calpeptin |
++
Calpain I (porcine erythrocytes), ID50: 52 nM Calpain II (porcine kidney), ID50: 40 nM |
98%+ | |||||||||||||||||
Cathepsin inhibitor 1 |
+++
Cathepsin L2, pIC50: 5.5 Cathepsin L, pIC50: 7.9 |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | 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] |
Dose | Mice: 1 mg/kg - 10 mg/kg[1] (p.o.,BID) |
Administration | p.o. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.06mL 0.41mL 0.21mL |
10.32mL 2.06mL 1.03mL |
20.64mL 4.13mL 2.06mL |
CAS号 | 1373215-15-6 |
分子式 | C25H29FN4O5 |
分子量 | 484.52 |
别名 | Z-FL-COCHO;Compound 5 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Store in freezer, under -20°C |
溶解度 |
DMSO: 50 mg/mL(103.19 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |