1. Metabolic Enzyme/Protease
  2. Cathepsin
  3. LY 3000328

LY 3000328 

Cat. No.: HY-15533 Purity: 99.35%
Handling Instructions

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

For research use only. We do not sell to patients.

LY 3000328 Chemical Structure

LY 3000328 Chemical Structure

CAS No. : 1373215-15-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 301 In-stock
Estimated Time of Arrival: December 31
5 mg USD 274 In-stock
Estimated Time of Arrival: December 31
10 mg USD 354 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1238 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

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

IC50 & Target

IC50: 7.7±5.85 nM (hCat S), 1.67±1.17 (mCat S)[1]

In Vitro

LY3000328 maintains excellent in vitro potency and selectivity. 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%). At a 100 μM concentration of LY3000328 there is only 6% displacement of [3H]-astemizole in an assay with HEK293 membrane preparation, indicating low potential of hERG blockade[1]. LY3000328 is a potent and specific inhibitor of cathepsin S (CatS). 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 features of the disease state in this model resemble those of human AAA. LY3000328 exhibits a dose-responsive aortic diameter reduction at 1, 3, 10, and 30 mg/kg. 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].

Clinical Trial
Molecular Weight

484.52

Formula

C₂₅H₂₉FN₄O₅

CAS No.

1373215-15-6

SMILES

O=C(C1=CC=C(F)C=C1)N[[email protected]@H]2[[email protected]@H](OC(NC)=O)COC3=CC=C(N4CCN(C5COC5)CC4)C=C32

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (103.19 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.16 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.16 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.16 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

LY 3000328LY3000328LY-3000328CathepsinInhibitorinhibitorinhibit

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Product Name:
LY 3000328
Cat. No.:
HY-15533
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