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Sacubitril

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Catalog No. T4574Cas No. 149709-62-6
Alias AHU-377, AHU377, AHU 377

Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM and is a component of the heart failure medicine LCZ696.

Sacubitril

Sacubitril

😃Good
Purity: 97.91%
Catalog No. T4574Alias AHU-377, AHU377, AHU 377Cas No. 149709-62-6
Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM and is a component of the heart failure medicine LCZ696.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$57In StockIn Stock
10 mg$77In StockIn Stock
25 mg$116In StockIn Stock
50 mg$147In StockIn Stock
100 mg$247In StockIn Stock
200 mg$368In StockIn Stock
500 mg$596-In Stock
1 mL x 10 mM (in DMSO)$63In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:97.91%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM and is a component of the heart failure medicine LCZ696.
Targets&IC50
NEP:5 nM 
In vitro
LCZ696 is a single molecule that is comprised of molecular moieties of valsartan, an ARB, and Sacubitril, a neprilysin inhibitor (1:1 ratio). Sacubitril is converted by enzymatic cleavage of the ethyl ester into the active neprilysin inhibiting metabolite LBQ657[2]. The inactive NEPi precursor, Sacubitril, does not inhibit collagen accumulation in fibroblasts nor cardiac myocyte hypertrophy. In cardiac fibroblasts, the active NEPi LBQ657 had no discernible effects. In contrast, LBQ657 modestly inhibits cardiac myocyte hypertrophy[3].
In vivo
In humans, Sacubitril (tmax0.5-1.1 h) are absorbed quickly. Sacubitril is converted rapidly into LBQ657 with its tmaxbeing reached in 1.9-3.5 h. Mean t1/2values for the biologically active LBQ657 is 9.9-11.1 h[2].In vehicle-treated dogs, ANF increases urinary sodium excretion from 17.3±3.6 to 199.5±18.4 pequivkglmin. This effect is potentiated significantly in animals which receive Sacubitril. Urinary volume is also potentiated in animals which receive an iv administration of Sacubitril[1].
SynonymsAHU-377, AHU377, AHU 377
Chemical Properties
Molecular Weight411.49
FormulaC24H29NO5
Cas No.149709-62-6
SmilesCCOC(=O)[C@H](C)C[C@@H](Cc1ccc(cc1)-c1ccccc1)NC(=O)CCC(O)=O
Relative Density.1.151 g/cm3 (Predicted)
Storage & Solubility Information
StoragePure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 27.5 mg/mL (66.83 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.86 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
1mg5mg10mg50mg
1 mM2.4302 mL12.1510 mL24.3019 mL121.5096 mL
5 mM0.4860 mL2.4302 mL4.8604 mL24.3019 mL
10 mM0.2430 mL1.2151 mL2.4302 mL12.1510 mL
20 mM0.1215 mL0.6075 mL1.2151 mL6.0755 mL
50 mM0.0486 mL0.2430 mL0.4860 mL2.4302 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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%
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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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