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    Sacubitril (AHU-377)
    Sacubitril (AHU-377)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V4539
    CAS #: 149709-62-6Purity ≥98%

    Description: Sacubitril (formerly known as AHU-377; Entresto) is a novel and potent NEP (neutral endopeptidase 24.11) inhibitor used in combination with valsartan (as LCZ696) for heart failure. It inhibits NEP with an IC50 of 5 nM. Sacubitril is a component of the heart failure medicine LCZ696 (sacubitril in combination with valsartan). Sacubitril is a prodrug that can be activated to LBQ657 by de-ethylation via esterases. LBQ657 inhibits the enzyme neprilysin, which is responsible for the degradation of atrial and brain natriuretic peptide, two blood pressure lowering peptides that work mainly by reducing blood volume.

    References: J Med Chem. 1995 May 12;38(10):1689-700.Expert Opin Investig Drugs. 2013 Aug;22(8):1041-7.Circ Heart Fail. 2015 Jan;8(1):71-8.

    Related CAS : 149709-62-6 (free acid); 1369773-39-6 (hemi-calcium); 149690-05-1 (sodium); 936623-90-4 (mixture with valsartan); 936623-90-4; 137862-53-4; 149709-44-4 (Sacubitrilat)

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    Sacubitril

    Molecular Weight: 411.49
    Formula: C₂₄H₂₉NO₅
    CAS No.: 149709-62-6
    SMILES: O=C(CCC(O)=O)N[[email protected]](CC1=CC=C(C2=CC=CC=C2)C=C1)C[[email protected]@H](C)C(OCC)=O
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: LCZ696; AHU377; LCZ 696; AHU 377; LCZ696; AHU-377; Entresto


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    In Vitro: To further examine the effect of sacubitril on cardiac fibrosis, we used TGF-β1 (10 ng/mL) to stimulate MEF for 24 h to induce a profibrotic phenotype. LBQ657, the metabolite of sacubitril, was used to treat MEF cells at a concentration of 50 µM prior to TGF-β1 stimulation. We found both the mRNA and protein expression of MMP9 and α-SMA was dramatically up-regulated by TGF-β1 stimulation, but this was prevented by LBQ657 pre-treatment (P < 0.01 comparison with the TGF-β1 group), indicating LBQ657 potently inhibited fibroblast activation in vitro.

    In Vivo: The rats were subcutaneous injected ISO to induce cardiac fibrosis and treated with normal saline, valsartan or sacubitril/valsartan, respectively (Figure 1A). Valsartan, a drug used for clinical treatment of heart failure, was used as positive control (Suematsu et al., 2016). The valsartan group and the sacubitril/valsartan group had lower heart weight to body weight ratio (Figure 1B). Echocardiogram showed that the cardiac output, ejection fraction, fractional shortening and stroke volume of ISO-induced rats were significantly increased after valsartan and sacubitril/valsartan treatment (Figures 1C,D). Especially, sacubitril/valsartan ameliorated stroke volume more efficiently than valsartan. Additionally, the valsartan group and the sacubitril/valsartan group had smaller area of fibrosis (Figure 1E) compared to non-treatment control group. These results indicate that sacubitril/valsartan effectively protected cardiac dysfunction in ISO-stimulated rats (P < 0.01 compared with control group)

    Formulation: sacubitril/valsartan group were given sacubitril valsartan by gavage (0.01 mL/g body weight, dissolved in 0.5% CMC-Na solution).

    References: Front Cell Dev Biol. 2021; 9: 760035.

    These protocols are for reference only. InvivoChem does not independently validate these methods.

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