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Umibecestat

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Catalog No. T13253Cas No. 1387560-01-1
Alias CNP520

Umibecestat is an inhibitor of beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1), with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively. Umibecestat can be used for the research of alzheimer's disease.

Umibecestat

Umibecestat

😃Good
Purity: 99.88%
Catalog No. T13253Alias CNP520Cas No. 1387560-01-1
Umibecestat is an inhibitor of beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1), with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively. Umibecestat can be used for the research of alzheimer's disease.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$175In StockIn Stock
5 mg$372In StockIn Stock
10 mg$538In StockIn Stock
25 mg$896In StockIn Stock
50 mg$1,220In StockIn Stock
100 mg$1,650-In Stock
1 mL x 10 mM (in DMSO)$418In StockIn 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:99.88%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Umibecestat is an inhibitor of beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1), with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively. Umibecestat can be used for the research of alzheimer's disease.
Targets&IC50
BACE1 (human):11 nM , BACE1 (mouse):10 nM
In vitro
Umibecestat is a potent inhibitor of BACE-1 that is selective for BACE-1 over other human pepsin-like aspartic proteases, including BACE-2 and cathepsin D[1].
In vivo
In both rat brain and CSF, Umibecestat (CNP520) (1.5-51.3 mg/kg; given by oral gavage; 72 hours) shows dose-dependent effects on Aβ40 and a long duration of action. Umibecestat (3.1 mg/kg; p.o.; 7 days) shows a > 75% reduction on Aβ40 and Aβ42 in CSF after dosing and returns slowly to baseline over the next 7 days[1].
SynonymsCNP520
Chemical Properties
Molecular Weight513.8
FormulaC19H15ClF7N5O2
Cas No.1387560-01-1
SmilesC[C@]1(CO[C@](C)(C(N)=N1)C(F)(F)F)c1nc(NC(=O)c2ncc(cc2Cl)C(F)(F)F)ccc1F
Relative Density.1.59 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 95 mg/mL (184.9 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9463 mL9.7314 mL19.4628 mL97.3141 mL
5 mM0.3893 mL1.9463 mL3.8926 mL19.4628 mL
10 mM0.1946 mL0.9731 mL1.9463 mL9.7314 mL
20 mM0.0973 mL0.4866 mL0.9731 mL4.8657 mL
50 mM0.0389 mL0.1946 mL0.3893 mL1.9463 mL
100 mM0.0195 mL0.0973 mL0.1946 mL0.9731 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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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2 Enter the in vivo formulation:
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Dose Conversion

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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

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