LCZ-696

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种新型单分子，包含缬沙坦和 NEP 抑制剂前药 AHU377 的分子部分。

A novel single molecule comprising molecular moieties of valsartan and NEP inhibitor prodrug AHU377 (1:1 ratio); causes dose-dependent increases in atrial natriuretic peptide immunoreactivity (due to NEP inhibition) in Sprague-Dawley rats and provides sustained, dose-dependent blood pressure reductions in hypertensive double-transgenic rats; orally active.Heart Failure Approved(In Vitro):Sacubitril/Valsartan (LCZ696; 1-30 μM; 0.5?hours) inhibits HG-treated H9C2 cells apoptosis in an experimental model of Diabetic cardiomyopathy (DCM).Sacubitril/Valsartan (1-30 μM; 0.5?hours) increases the expression level of cleaved caspase-3 and the ratio of Bax/Bcl-2 in HG-treated H9C2 cells.(In Vivo):Sacubitril/Valsartan (LCZ696; perorally; 68 mg/kg for 4 weeks) significantly exhibits small weights and reduces interstitial fibrosis both in the noninfarct zone and peri-infarct zone.

Sacubitril/Valsartan (LCZ696; 1-30 μM; 0.5?hours) inhibits HG-treated H9C2 cells apoptosis in an experimental model of Diabetic cardiomyopathy (DCM). Sacubitril/Valsartan (1-30 μM; 0.5?hours) increases the expression level of cleaved caspase-3 and the ratio of Bax/Bcl-2 in HG-treated H9C2 cells. Apoptosis Analysis Cell Line:HG-treated H9C2 cells Concentration:1, 10, or 30 μM Incubation Time:0.5?hours Result:Inhibited HG-treated H9C2 cells apoptosis.Western Blot AnalysisCell Line:HG-treated H9C2 cells Concentration:1, 10, or 30 μM Incubation Time:0.5?hours Result:Increased the expression level of cleaved caspase-3 and the ratio of Bax/Bcl-2.

Sacubitril/Valsartan (LCZ696; perorally; 68 mg/kg for 4 weeks) significantly exhibits small weights and reduces interstitial fibrosis both in the noninfarct zone and peri-infarct zone. Animal Model:Adult 6- to 8-week-old male Sprague-Dawley rats (220-250 g body weight) Dosage:68 mg/kg Administration:Perorally; for 4 weeks Result:Exhibited small weights and reduced interstitial fibrosis both in the noninfarct zone and peri-infarct zone.

LCZ696 | LCZ 696

Metabolic Enzyme/Protease

Neprilysin

RAAS

Cardiovascular Disease

——

936623-90-4

957.99

C48H60N6Na3O10.5

>98% (HPLC)

10 mM in DMSO

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

L-Valine, N-(1-oxopentyl)-N-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-, 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)

(-20℃)

With Ice Pack

≥ 2 years