A dual angiotensin II receptor antagonist and neprilysin inhibitor
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LCZ696

Item No. 23425

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(1-oxopentyl)-N-[[2’-(2H-tetrazol-5-yl)[1,1’-biphenyl]-4-yl]methyl]-L-valine compd. with α-ethyl (αR,γS)-γ-[(3-carboxy-1-oxopropyl)amino]-α-methyl[1,1’-biphenyl]-4-pentanoate, sodium salt, hydrate (2:2:6:5)
CAS Number
936623-90-4
Molecular Formula
C24H29N5O3 • C24H29NO5 • 5/2H2O • 3Na
Formula Weight
916.0
Purity
≥98% (1:1 ratio of Valsartan and AHU377)
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 20 mg/mlEthanol: 30 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
251 nm
SMILES
O=C(CCCC)N([C@H](C(O)=O)C(C)C)CC1=CC=C(C2=CC=CC=C2C3=NNN=N3)C=C1.C[C@@H](C(OCC)=O)C[C@H](NC(CCC(O)=O)=O)CC(C=C4)=CC=C4C5=CC=CC=C5.O.O.O.[Na].[Na].[Na]
InChi Code
InChI=1S/C24H29N5O3.C24H29NO5.3Na.9H2O/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,(H,31,32)(H,25,26,27,28);4-12,17,21H,3,13-16H2,1-2H3,(H,25,26)(H,27,28);;;;9*1H2/t22-;17-,21+;;;;;;;;;;;;/m01............/s1
InChi Key
YYXACTPPFJVFTL-DKPGDUSBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $41

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    25 mg

    $80

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    50 mg

    $128

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    Product Description

    LCZ696 is a dual angiotensin II receptor antagonist and neprilysin inhibitor that is a combination of the nonpeptide angiotensin II receptor antagonist valsartan (Item No. 14178) and AHU377 (Item No. 21473), a prodrug of LBQ657 (Item No. 19829), which is an inhibitor of the zinc metallopeptidase neprilysin.1,2,3 LCZ696 (2-60 mg/kg) induces a dose-dependent decrease in mean arterial pressure in rats expressing human renin and angiotensinogen, a double-transgenic model for angiotensin II-dependent hypertension.3 Formulations containing LCZ696 have been used in the treatment of chronic heart failure.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Burnier, M. Angiotensin II type 1 receptor blockers. Circulation 103(6), 904-912 (2001).

    2. Schiering, N., D'Arcy, A., Villard, F., et al. Structure of neprilysin in complex with the active metabolite of sacubitril. Sci. Rep. 6, 27909 (2016).

    3. Gu, J., Noe, A., Chandra, P., et al. Pharmacokinetics and pharmacodynamics of LCZ696, a novel dual-acting angiotensin receptor-neprilysin inhibitor (ARNi). J. Clin. Pharmacol. 50(4), 401-414 (2010).