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LY 3000328

Catalog No. TQ0116 CAS 1373215-15-6

Synonyms: Cathepsin S inhibitor

LY 3000328 (Cathepsin S inhibitor) is a potent, highly selective Cathepsin S (Cat S) inhibitor (IC50s: 7.7 and 1.67 nM for hCat S and mCat S).

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LY 3000328, CAS 1373215-15-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 97.00
2 mg	In stock	$ 139.00
5 mg	In stock	$ 221.00
10 mg	In stock	$ 292.00
25 mg	In stock	$ 513.00
50 mg	In stock	$ 746.00
100 mg	In stock	$ 1,050.00
1 mL * 10 mM (in DMSO)	In stock	$ 231.00

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Purity: 99.01%

Purity: 97.83%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	LY 3000328 (Cathepsin S inhibitor) is a potent, highly selective Cathepsin S (Cat S) inhibitor (IC50s: 7.7 and 1.67 nM for hCat S and mCat S).
Targets&IC50	Cathepsin S (mouse):1.67 nM, Cathepsin S (human):7.7 nM
In vitro	LY3000328 shows low in vitro CYP450 inhibition (<15% at 10 μM for CYP3A4, CYP2D6, and CYP2C9); low in vitro metabolism in mouse, rat, dog, and human liver microsomes (<20% after 30 min incubation at 4 μM); and good permeability (MDCK A-B>4%) [1]. LY3000328 is a potent and specific inhibitor of cathepsin S (CatS). The inhibition of CatS activity in plasma would be 50% of maximal when LY3000328 plasma concentration is approximately 60 ng/mL [2].
In vivo	The efficacies of LY3000328 is studied in a mouse model of abdominal aortic aneurysm (AAA). In this model, inflammation is induced using CaCl2 applied to the ablumenal surface. It is shown that the features of the disease state in this model resemble those of human AAA. LY3000328 (1, 3, 10, 30 mg/kg) exhibits a dose-responsive aortic diameter reduction. At the lowest dose of 1 mg/kg of LY3000328, the aortic diameter is reduced by 58%, then 83% at 3 mg/kg, and 87% at 10 mg/kg. The exposure (AUC) for both compounds increased in a dose-dependent manner, suggesting that the drug disposition properties of LY3000328 are favorable [1].

Synonyms	Cathepsin S inhibitor
Molecular Weight	484.52
Formula	C25H29FN4O5
CAS No.	1373215-15-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 48 mg/mL (99.06 mM)

References and Literature

1. Jadhav PK, 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, et al. Pharmacokinetics and pharmacodynamics of the cathepsin S inhibitor, LY3000328, in healthy subjects. Br J Clin Pharmacol. 2014 Dec;78(6):1334-42.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compounds Library Max Protease Inhibitor Library ReFRAME Related Library Bioactive Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

LY 3000328 1373215-15-6 Proteases/Proteasome Cysteine Protease Cathepsin S inhibitor Cathepsin Inhibitor inhibit LY3000328 LY-3000328 inhibitor

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