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LY 3000328

Catalog No. TQ0116Cas No. 1373215-15-6
Alias Cathepsin S inhibitor

LY 3000328 (Cathepsin S inhibitor) is a selective inhibitor of cathepsin S with IC50 values ​​of 7.7 and 1.67 nM for human and mouse cathepsin S, respectively. LY 3000328 (Cathepsin S inhibitor) may slow or prevent abdominal aortic aneurysm (AAA) expansion and/or reduce the risk of AAA rupture by inhibiting cathepsin S-mediated degradation of extracellular matrix proteins, elastin and collagen.

LY 3000328

LY 3000328

Purity: 99.01%
Catalog No. TQ0116Alias Cathepsin S inhibitorCas No. 1373215-15-6
LY 3000328 (Cathepsin S inhibitor) is a selective inhibitor of cathepsin S with IC50 values ​​of 7.7 and 1.67 nM for human and mouse cathepsin S, respectively. LY 3000328 (Cathepsin S inhibitor) may slow or prevent abdominal aortic aneurysm (AAA) expansion and/or reduce the risk of AAA rupture by inhibiting cathepsin S-mediated degradation of extracellular matrix proteins, elastin and collagen.
Pack SizePriceAvailabilityQuantity
1 mg$97In Stock
2 mg$139In Stock
5 mg$221In Stock
10 mg$292In Stock
25 mg$513In Stock
50 mg$746In Stock
100 mg$1,050In Stock
1 mL x 10 mM (in DMSO)$231In Stock
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Purity:99.01%
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Product Introduction

Bioactivity
Description
LY 3000328 (Cathepsin S inhibitor) is a selective inhibitor of cathepsin S with IC50 values ​​of 7.7 and 1.67 nM for human and mouse cathepsin S, respectively. LY 3000328 (Cathepsin S inhibitor) may slow or prevent abdominal aortic aneurysm (AAA) expansion and/or reduce the risk of AAA rupture by inhibiting cathepsin S-mediated degradation of extracellular matrix proteins, elastin and collagen.
Targets&IC50
Cathepsin S (mouse):1.67 nM, Cathepsin S (human):7.7 nM
In vitro
METHODS: The activity of LY 3000328 (Cathepsin S inhibitor) was evaluated in hCat S and mCat S enzyme inhibition assays.
RESULTS The IC50 values ​​of LY 3000328 (Cathepsin S inhibitor) for inhibiting human and mouse Cat S were 7.7±5.85 and 1.67±1.17 nM, respectively. [1]
In vivo
METHODS: The efficacy of LY 3000328 (Cathepsin S inhibitor)(1, 3, 10, 30 mg/kg, oral, 28 days) in BID mice was studied.
RESULTS When the lowest dose of LY 3000328 (Cathepsin S inhibitor) was 1 mg/kg, the aortic diameter decreased by 58%, 83% at 3 mg/kg, and 87% at 10 mg/kg; the exposure (AUC) of LY 3000328 (Cathepsin S inhibitor) increased in a dose-dependent manner, indicating good drug disposition performance. [1]
AliasCathepsin S inhibitor
Chemical Properties
Molecular Weight484.52
FormulaC25H29FN4O5
Cas No.1373215-15-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 48 mg/mL (99.06 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0639 mL10.3195 mL20.6390 mL103.1949 mL
5 mM0.4128 mL2.0639 mL4.1278 mL20.6390 mL
10 mM0.2064 mL1.0319 mL2.0639 mL10.3195 mL
20 mM0.1032 mL0.5160 mL1.0319 mL5.1597 mL
50 mM0.0413 mL0.2064 mL0.4128 mL2.0639 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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