LY 3000328

SKU: orb1296192

Description

LY 3000328 is a potent and selective cathepsin S inhibitor, with IC50 values of 7.7 nM (human) and 1.67 nM (mouse). It is a research tool for studying extracellular matrix remodeling, with applications in investigating abdominal aortic aneurysm (AAA) progression in preclinical models through the inhibition of elastin and collagen degradation.

Research Area

Protein Biochemistry

Images & Validation

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Key Properties

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CAS Number	1373215-15-6
MW	484.52
Purity	99.54% (May vary between batches)
Formula	C₂₅H₂₉FN₄O₅
SMILES	CNC(=O)O[C@H]1COc2ccc(cc2[C@@H]1NC(=O)c1ccc(F)cc1)N1CCN(CC1)C1COC1
Target	Cysteine Protease
Solubility	DMSO:62.5 mg/mL (128.99 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.13 mM)

Bioactivity

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Target IC50	Cathepsin S (mouse):1.67 nM\|Cathepsin S (human):7.7 nM
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. Read more...
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. Read more...

Storage & Handling

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Storage	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Cathepsin, Cathepsin S, Cathepsin S inhibitor, CysteineProtease, Cysteine Protease, inhibit, LY 3000328, LY3000328, LY-3000328, Inhibitor

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Compound Identifiers

PubChem CID

67475270 ↗

Key Properties

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No computed properties available.

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LY 3000328

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Quality Guarantee

Compound Identifiers

Key Properties

Documents Download

Request a Document

Protocol Information

LY 3000328 (orb1296192)

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