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CAS No.: 1373215-15-6

LY 3000328 Catalog No. CSN17758

Synonyms: Z-FL-COCHO;Cathepsin S Inhibitor

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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400-920-2911

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生物活性

实验方案

技术信息

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]
动物研究
剂量
Mice: 1 mg/kg - 10 mg/kg^[1] (p.o.,BID)

给药途径
p.o.
临床研究

动物研究
剂量	Mice: 1 mg/kg - 10 mg/kg^[1] (p.o.,BID)
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01515358	Healthy Volunteers	Phase 1	Completed	-	Singapore ... more >> For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Singapore, Singapore, 117597 Collapse <<

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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0639 mL
- 10.3195 mL
- 20.6390 mL
- 5 mM
- 0.4128 mL
- 2.0639 mL
- 4.1278 mL
- 10 mM
- 0.2064 mL
- 1.0319 mL
- 2.0639 mL

技术信息

CAS号

1373215-15-6

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H29FN4O5

运输

蓝冰

分子量

484.52

别名

Z-FL-COCHO;Cathepsin S Inhibitor

溶解度

DMSO	265.0 mg/mL (546.9 mM)
Water	insoluble

动物实验配方

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