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Sacubitril/Valsartan

(Synonyms: 沙库必曲/缬沙坦; LCZ696)

目录号: PL04787 纯度: ≥99%

Sacubitril/Valsartan (LCZ696) 是由 Valsartan (an ARB) 和 Sacubitril (AHU377) 组成，摩尔比为 1:1，是一种首创的，口服有效的血管紧张素受体-脑啡肽酶 (ARN) 双抑制剂，用于研究高血压和心力衰竭。Sacubitril/Valsartan 可通过抑制炎症、氧化应激和细胞凋亡来改善糖尿性心肌病。

CAS No. :936623-90-4

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中文名称	Sacubitril/Valsartan
中文别名	LCZ696 抑制剂;LCZ696杂质;LCZ696中间体9;Sacubitril诺华心衰药Entresto(LCZ696);沙库必曲 LCZ696;奥帕曲拉;诺华心衰药ENTRESTO(LCZ696);沙库比曲;沙库比曲缬沙坦共晶体;沙库必曲;缬沙坦;缬沙坦片;LCZ696;沙库必曲缬沙坦钠盐;奥帕曲拉/缬沙坦;萨库比尔杂质1;沙库必曲缬沙坦钠;塞可比曲缬沙坦;沙库必曲缬沙坦钠(LCZ696);沙卡布曲缬沙坦SACUBITRIL/VALSARTAN;沙库必曲/缬沙坦
英文名称	Sacubitril/Valsartan
英文别名	Sacubitril;3-(1-Biphenyl-4-ylMethyl-3-ethoxycarbonyl-1-butylcarbaMoyl)propionate-3'-Methyl-2'-(pentanoyl(2'-(tetrazol-5-ylate)biphenyl-4'-ylMethyl)aMino)butyrate;(S)-2-(N-((2'-(1H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)hexanamido)-3-methylbutanoic acid compound with 4-(((2S,4R)-1-([1,1'-biphenyl]-4-yl)-5-ethoxy-4-me;Entresto(LCZ696);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];LCZ 696;LCZ-696;LCZ696 Entresto TM;Valsartan;BAL-4815;Isavuconazole;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);RO-0094815;trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl)propionate-(S)-3-methyl-2-(pentanoyl{2”-(tetrazol-5-ylate)biphenyl-4-ylmethyl}amino)butyrate] hemipentahydrate;trisodium 3-((1S,3R)-1-(biphenyl-4-ylme;Sacubitril valsartan sodium hydrate;LCZ696;Entresto;LZC696;[(C24H29N5O3).(C24H29NO5).2.5(H2O).3Na];LCZ696 ENTRESTO TM;LCZ696 Entresto;4-[[(2S,4R)-5-ethoxy-4-methyl-5-oxo-1-(4-phenylphenyl)pentan-2-yl]amino]-4-oxobutanoate;Sacubitril mixture with Valsartan;Cocrystal of Sacubitril and Valsartan;Sacubitril/Valsartan;Neparvis;Sacubitril-valsartan;Sacubitril-valsartan mixt.;Valsartan sacubitril
Cas No.	936623-90-4
分子式	C₄₈H₆₁N₆NaO₉
分子量	889.02
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述	Sacubitril/Valsartan (LCZ696) 是由 Valsartan (an ARB) 和 Sacubitril (AHU377) 组成，摩尔比为 1:1，是一种首创的，口服有效的血管紧张素受体-脑啡肽酶 (ARN) 双抑制剂，用于研究高血压和心力衰竭。Sacubitril/Valsartan 可通过抑制炎症、氧化应激和细胞凋亡来改善糖尿性心肌病。

产品详情

生物活性

Sacubitril/Valsartan (LCZ696), comprised Valsartan and Sacubitril (AHU377) in 1:1 molar ratio, is a first-in-class, orally bioavailable, and dual-acting angiotensin receptor-neprilysin (ARN) inhibitor for hypertension and heart failure. Sacubitril/Valsartan ameliorates diabetic cardiomyopathy by inhibiting inflammation, oxidative stress and apoptosis.

性状

Solid

IC50 & Target[1][2]

Angiotensin receptor-neprilysin

体外研究(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.
has not independently confirmed the accuracy of these methods. They are for reference only.Apoptosis Analysis

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Gu J, 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.
[2]. von Lueder TG, 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.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (104.39 mM)H₂O : ≥ 50 mg/mL (52.19 mM)

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Sacubitril/Valsartan

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