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LCZ696(Sacubitril-Valsartan)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LCZ696(Sacubitril-Valsartan)图片
CAS NO:936623-90-4
规格:≥98%
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
5g电议

产品介绍
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.
理化性质和储存条件
Molecular Weight (MW)915.98
FormulaC24H29N5O3.C24H29NO5.5/2H2O.3Na
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 Key: UOLUPHRXIRFONO-JOYYXRJNSA-K
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)[C@@H](C([O-])=O)N(C(CCCC)=O)CC1=CC=C(C2=CC=CC=C2C3=NN=N[N-]3)C=C1.O=C(OCC)[C@H](C)C[C@H](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.
实验参考方法
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.