2. Metabolic Enzyme/Protease
  3. Neprilysin
  4. Sacubitril

Sacubitril (AHU-377) is a potent and orally active NEP (neprilysin) inhibitor with an IC50 of 5 nM. Sacubitril is a component of the heart failure medicine LCZ696. Sacubitril can be used for the research of heart failure, hypertension and COVID-19.

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

CAS No. : 149709-62-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Sacubitril:

Sacubitril Related Antibodies

Top Publications Citing Use of Products

    Sacubitril purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Aug 11;11(18):8797-8812.

    N2a-APP cells were treated with Diosmin (Dio; 80 μM), FICZ (250 nM), L-KN (3 μM) or Indole-3-acetamide (I3C; 10 μM) with or without SR1 (2 μM) or Sacubitril (Sac; 1 μM) for 24 h, the supernatant was collected and the Aβ42 levels were determined by ELISA.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Sacubitril (AHU-377) is a potent and orally active NEP (neprilysin) inhibitor with an IC50 of 5 nM. Sacubitril is a component of the heart failure medicine LCZ696. Sacubitril can be used for the research of heart failure, hypertension and COVID-19[1][2][3].

    IC50 & Target

    IC50: 5 nM (NEP)[1]
    In Vitro

    Sacubitril (AHU-377) is a single molecule that is comprised of molecular moieties of valsartan, an ARB, and Sacubitril (AHU-377), a neprilysin inhibitor (1:1 ratio). Sacubitril (AHU-377) is converted by enzymatic cleavage of the ethyl ester into the active neprilysin inhibiting metabolite LBQ657[2].
    The inactive NEPi precursor, Sacubitril (AHU-377), 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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Sacubitril Related Antibodies
    In Vivo

    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 (AHU-377). Urinary volume is also potentiated in animals which receive an iv administration of Sacubitril (AHU-377)[1].
    In normotensive rats, pretreatment with Sacubitril (3, 10 and 30 mg/kg, PO.) augments ANP-evoked plasma cGMP levels by 2.4, 3.3 and 4.0 fold, respectively (4h AUC compared to vehicle)[4].
    Sacubitril (30 and 100 mg/kg, PO) produces a dose-dependent antihypertensive effect in Dahl-SS rats[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    411.49

    Formula

    C24H29NO5
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C(CCC(O)=O)N[C@H](CC1=CC=C(C2=CC=CC=C2)C=C1)C[C@@H](C)C(OCC)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 75 mg/mL (182.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4302 mL 12.1510 mL 24.3019 mL
    5 mM 0.4860 mL 2.4302 mL 4.8604 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: ≥ 2.5 mg/mL (6.08 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (6.08 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.92%

    SDS (393 KB)

    COA (249 KB) LCMS (96 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.4302 mL 12.1510 mL 24.3019 mL 60.7548 mL
    5 mM 0.4860 mL 2.4302 mL 4.8604 mL 12.1510 mL
    10 mM 0.2430 mL 1.2151 mL 2.4302 mL 6.0755 mL
    15 mM 0.1620 mL 0.8101 mL 1.6201 mL 4.0503 mL
    20 mM 0.1215 mL 0.6075 mL 1.2151 mL 3.0377 mL
    25 mM 0.0972 mL 0.4860 mL 0.9721 mL 2.4302 mL
    30 mM 0.0810 mL 0.4050 mL 0.8101 mL 2.0252 mL
    40 mM 0.0608 mL 0.3038 mL 0.6075 mL 1.5189 mL
    50 mM 0.0486 mL 0.2430 mL 0.4860 mL 1.2151 mL
    60 mM 0.0405 mL 0.2025 mL 0.4050 mL 1.0126 mL
    80 mM 0.0304 mL 0.1519 mL 0.3038 mL 0.7594 mL
    100 mM 0.0243 mL 0.1215 mL 0.2430 mL 0.6075 mL
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    Sacubitril Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Sacubitril149709-62-6AHU-377AHU377AHU 377NeprilysinNeutral endopeptidaseNEPCluster of differentiation 10CD10COVID-19neutral endopeptidasenatriuretic peptideantihypertensiveheart failureInhibitorinhibitorinhibit

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