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    LCZ696 (Sacubitril-Valsartan)
    LCZ696  (Sacubitril-Valsartan)

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    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V1778
    CAS #: 936623-90-4Purity ≥98%

    Description: LCZ696 (LCZ-696; LCZ 696; Entresto; Sacubitril mixture with Valsartan), the combination of valsartan with sacubitril in 1:1 molar ratio, is an orally bioavailable and dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) approved in 2015 for the treatment of hypertension and heart failure. 

    References: J Clin Pharmacol. 2010 Apr;50(4):401-14; Circ Heart Fail. 2015 Jan;8(1):71-8.

    Related CAS#: 137862-53-4 (Valsartan); 149690-05-1 (Valsartan sodium)  

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    • 香港大学
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    Molecular Weight (MW)915.98
    CAS No.936623-90-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 30 mg/mL warmed (32.8 mM)
    Water: 100 mg/mL (109.2 mM)
    Ethanol: 9 mg/mL (9.8 mM)
    Other infoChemical Name: sodium (S)-5-(4'-((N-(1-carboxylato-2-methylpropyl)pentanamido)methyl)-[1,1'-biphenyl]-2-yl)tetrazol-1-ide 4-(((2S,4R)-1-([1,1'-biphenyl]-4-yl)-5-ethoxy-4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoate hydrate
    InChi Code: InChI=1S/C24H29N5O3.C24H29NO5.3Na.H2O/c1-4-5-10-21(30)29(22(16(2)3)24(31)32)15-17-11-13-18(14-12-17)19-8-6-7-9-20(19)23-25-27-28-26-23;1-3-30-24(29)17(2)15-21(25-22(26)13-14-23(27)28)16-18-9-11-20(12-10-18)19-7-5-4-6-8-19;;;;/h6-9,11-14,16,22H,4-5,10,15H2,1-3H3,(H2,25,26,27,28,31,32);4-12,17,21H,3,13-16H2,1-2H3,(H,25,26)(H,27,28);;;;1H2/q;;3*+1;/p-3/t22-;17-,21+;;;;/m01..../s1
    SMILES Code: CC(C)[[email protected]@H](C([O-])=O)N(C(CCCC)=O)CC1=CC=C(C2=CC=CC=C2C3=NN=N[N-]3)C=C1.O=C(OCC)[[email protected]](C)C[[email protected]](NC(CCC([O-])=O)=O)CC4=CC=C(C5=CC=CC=C5)C=C4.[Na+].[Na+].[Na+].O
    Synonymsvalsartan / sacubitril (1:1); LCZ-696; LCZ696; LCZ 696; trade name: Entresto.

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    In Vitro

    In vitro activity: LCZ696 exerts a blood pressure lowering effect. Blood pressure reduction by LCZ696 is associated with a significant increase in urinary sodium excretion and sympathetic activity suppression. LCZ696 significantly ameliorates cardiac hypertrophy and inflammation, coronary arterial remodeling, and vascular endothelial dysfunction in high-salt loaded SHRcp compared with valsartan.

    Cell Assay: The neprilysin inhibitor component of LCZ696, LBQ657, inhibits hypertrophy but not fibrosis. The angiotensin receptor blocker component of LCZ696, valsartan inhibits both hypertrophy and fibrosis. Dual valsartan+LBQ augment the inhibitory effects of valsartan and the highest doses completely abrogate angiotensin II-mediated effects. Pre-treatment with LCZ696 reduces the ischemic area. The decrease in cerebral blood flow in the peripheral region of the ischemic area is significantly attenuated by pre-treatment with LCZ696. LCZ696 pre-treatment significantly decreases the increase of superoxide anion production in the cortex on the ischemic side. 

    In VivoIn double-transgenic rats overexpressing human renin and angiotensinogen and plasma atrial natriuretic peptide immunoreactivity, LCZ696 (60 mg/kg p.o.) induces a dose-dependent and long-lasting reduction in mean arterial pressure (MAP), and stimulates a rapid and dose-dependent augmentation of plasma ANP immunoreactivity. In rat myocardial infarction (MI) model, LCZ696 (68 mg/kg p.o.) attenuates cardiac remodeling and dysfunction after myocardial infarction by reducing cardiac fibrosis and hypertrophy. 
    Animal modelRats
    Formulation & Dosage60 mg/kg p.o.
    ReferencesJ Clin Pharmacol. 2010 Apr;50(4):401-14; Circ Heart Fail. 2015 Jan;8(1):71-8.

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


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