产品说明书

LY 3000328

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Chemical Structure| 1373215-15-6 同义名 : Z-FL-COCHO;Compound 5
CAS号 : 1373215-15-6
货号 : A473978
分子式 : C25H29FN4O5
纯度 : 99%+
分子量 : 484.52
MDL号 : MFCD28502827
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
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：
生物活性
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]
实验方案
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
参考文献

[1]Jadhav PK, Schiffler MA, et al. Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. ACS Med Chem Lett. 2014 Aug 27;5(10):1138-42.

[2]Payne CD, Deeg MA, et al. Pharmacokinetics and pharmacodynamics of the cathepsin S inhibitor, LY3000328, in healthy subjects. Br J Clin Pharmacol. 2014 Dec;78(6):1334-42.