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LY 3000328

Name: LY 3000328
Brand: TargetMol
SKU: TQ0116
Price: 97 USD
Availability: InStock
Rating: 5 (10 reviews)

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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

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Purity: 99.54%

Catalog No. TQ0116Alias Cathepsin S inhibitorCas No. 1373215-15-6

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$97	In Stock	In Stock
2 mg	$139	In Stock	In Stock
5 mg	$221	In Stock	In Stock
10 mg	$292	In Stock	In Stock
25 mg	$513	In Stock	In Stock
50 mg	$746	In Stock	In Stock
100 mg	$1,050	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$231	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.54%

Appearance:Solid

Color:White

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COA LCMS HNMR

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]
Synonyms	Cathepsin S inhibitor

Chemical Properties

Molecular Weight	484.52
Formula	C₂₅H₂₉FN₄O₅
Cas No.	1373215-15-6
Smiles	CNC(=O)O[C@H]1COc2ccc(cc2[C@@H]1NC(=O)c1ccc(F)cc1)N1CCN(CC1)C1COC1
Relative Density.	1.38 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 62.5 mg/mL (128.99 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.13 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0639 mL	10.3195 mL	20.6390 mL	103.1949 mL
5 mM	0.4128 mL	2.0639 mL	4.1278 mL	20.6390 mL
10 mM	0.2064 mL	1.0319 mL	2.0639 mL	10.3195 mL
20 mM	0.1032 mL	0.5160 mL	1.0319 mL	5.1597 mL
50 mM	0.0413 mL	0.2064 mL	0.4128 mL	2.0639 mL
100 mM	0.0206 mL	0.1032 mL	0.2064 mL	1.0319 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

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