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LY 3000328

Catalog No. TQ0116 CAS 1373215-15-6

Synonyms: Cathepsin S inhibitor

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

LY 3000328, CAS 1373215-15-6

Pack Size	Availability	Price/USD
1 mg	In stock	118.00
5 mg	In stock	221.00
10 mg	In stock	322.00
25 mg	In stock	570.00
50 mg	In stock	943.00
100 mg	In stock	1448.00
1 mL * 10 mM (in DMSO)	In stock	231.00

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Purity 99.01%

HNMR HPLC COA

Purity 97.83%

HNMR HPLC COA

Datasheet SDS

Biological Description

Chemical Properties

Storage & Solubility Information

Description

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

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
Purity	99.01%
Molecular Weight	484.52
Formula	C25H29FN4O5
CAS No.	1373215-15-6

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 6 months

Solubility Information

DMSO: 48 mg/mL (99.06 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

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：

Bioactive Compound Library Inhibitor Library

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LY 3000328 Aurantiamide acetate 2-Cyanopyrimidine Z-FA-FMK MG-101 E 64c Leupeptin Hemisulfate Calpeptin

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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.

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.