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沙库必曲/缬沙坦 /Sacubitril/Valsartan {[allProObj[0].p_purity_real_show]}

货号:A163102 同义名: LCZ 696;Sacubitril

LCZ 696 is a mixture of neprilysin inhibitor sacubitril and the angiotensin receptor blocker valsartan in a ratio of 1:1.

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Sacubitril/Valsartan 化学结构 CAS号:936623-90-4
Sacubitril/Valsartan 化学结构
CAS号:936623-90-4
Sacubitril/Valsartan 3D分子结构
CAS号:936623-90-4
Sacubitril/Valsartan 化学结构 CAS号:936623-90-4
Sacubitril/Valsartan 3D分子结构 CAS号:936623-90-4
规格 价格 会员价 库存 数量
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Sacubitril/Valsartan 纯度/质量文件 产品仅供科研

货号:A163102 标准纯度: {[allProObj[0].p_purity_real_show]}
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Sacubitril/Valsartan 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].

Sacubitril/Valsartan 动物研究

Dose Mice: 60 mg/kg[3] (p.o.), 6 mg/kg[4] (p.o.) Rat: 2 mg/kg - 60 mg/kg[5] (p.o.) Beagle dog: 15 mg/kg, 45 mg/kg[6] (p.o.)
Administration p.o.

Sacubitril/Valsartan 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.

Sacubitril/Valsartan 实验方案

计算器
存储液制备 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

Sacubitril/Valsartan 技术信息

CAS号936623-90-4
分子式C96H120N12Na6O21
分子量 1915.986
别名 LCZ 696;Sacubitril;LCZ 696. valsartan / sacubitril (1:1). Brand name: Entresto.;Valsartan
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

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
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