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Proteases/Proteasome Cysteine Protease LY 3000328

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 Quantity
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%
Purity 97.83%
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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