产品说明书

Sacubitril/Valsartan

Print
Chemical Structure| 936623-90-4 同义名 : LCZ 696;Sacubitril;LCZ 696. valsartan / sacubitril (1:1). Brand name: Entresto.;Valsartan
CAS号 : 936623-90-4
货号 : A163102
分子式 : C96H120N12Na6O21
纯度 : 98%
分子量 : 1915.986
MDL号 : MFCD28167829
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(54.8 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(26.1 mM)
动物实验配方：
生物活性
靶点

  • RAAS
描述 Angiotensin receptor blockade and neprilysin (NEP) inhibition together offer potential benefits for the treatment of hypertension and heart failure. LCZ696, composed of valsartan and sacubitril with a molar ratio of 1:1, is an oral bioactive, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for the treatment of hypertension and heart failure[3]. H9C2 cells were pretreated with LCZ696 at concentrations of 1, 10, or 30 μM for 30 min and then stimulated with high glucose (HG) for 48 h. HG- or diabetes-induced JNK/p38MAPK phosphorylation and NF-kB nuclear translocation were inhibited by the administration of LCZ696[4]. Oral administration of LCZ696 caused dose-dependent increases in atrial natriuretic peptide immunoreactivity (due to NEP inhibition) in Sprague-Dawley rats and provided sustained, dose-dependent blood pressure reductions in hypertensive double-transgenic rats[3]. Adult male Sprague–Dawley rats were randomized to treatment for 4 weeks with LCZ696 (68 mg/kg body weight perorally; myocardial infarction (MI) -ARNi, n=11), and the degree of fibrosis both in noninfarcted remote myocardium and in the peri-infarct zone was significantly reduced[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

0.52mL

0.10mL

0.05mL

2.61mL

0.52mL

0.26mL

5.22mL

1.04mL

0.52mL
参考文献

[1]von Lueder TG, Wang BH, et al. Angiotensin receptor neprilysin inhibitor LCZ696 attenuates cardiac remodeling and dysfunction after myocardial infarction by reducing cardiac fibrosis and hypertrophy. Circ Heart Fail. 2015 Jan;8(1):71-8.

[2]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. 2010 Apr;50(4):401-14.

[3]Gu J, Noe A, Chandra P, Al-Fayoumi S, Ligueros-Saylan M, Sarangapani R, Maahs S, Ksander G, Rigel DF, Jeng AY, Lin TH, Zheng W, Dole WP. Pharmacokinetics and pharmacodynamics of LCZ696, a novel dual-acting angiotensin receptor-neprilysin inhibitor (ARNi). J Clin Pharmacol. 2010 Apr;50(4):401-14. doi: 10.1177/0091270009343932. Epub 2009 Nov 23. PMID: 19934029.

[4]Ge Q, Zhao L, Ren XM, Ye P, Hu ZY. LCZ696, an angiotensin receptor-neprilysin inhibitor, ameliorates diabetic cardiomyopathy by inhibiting inflammation, oxidative stress and apoptosis. Exp Biol Med (Maywood). 2019 Sep;244(12):1028-1039. doi: 10.1177/1535370219861283. Epub 2019 Jul 1. PMID: 31262190; PMCID: PMC6879777.

[5]von Lueder TG, Wang BH, Kompa AR, Huang L, Webb R, Jordaan P, Atar D, Krum H. Angiotensin receptor neprilysin inhibitor LCZ696 attenuates cardiac remodeling and dysfunction after myocardial infarction by reducing cardiac fibrosis and hypertrophy. Circ Heart Fail. 2015 Jan;8(1):71-8. doi: 10.1161/CIRCHEARTFAILURE.114.001785. Epub 2014 Oct 31. PMID: 25362207.