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• 产品描述： 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

• 靶点： Angiotensin receptor-neprilysin;Apoptosis; RAAS; Neprilysin

• 体外研究：
  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 Analysis Cell 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.

• 体内研究：
  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.

• 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. 3. Huo H, et al. Erastin Disrupts Mitochondrial Permeability Transition Pore (mPTP) and Induces Apoptotic Death of Colorectal Cancer Cells. PLoS One. 2016 May 12;11(5):e0154605. 4. Ge Q, et al. Feature article: LCZ696, an angiotensin receptor-neprilysin inhibitor, ameliorates diabeticcardiomyopathy by inhibiting inflammation, oxidative stress and apoptosis. Exp Biol Med (Maywood). 2019 Sep;244(12):1028-1039.

• 溶解性： Soluble  in  DMSO、H2O

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.044 ml	5.219 ml	10.439 ml
  5 mM	0.209 ml	1.044 ml	2.088 ml
  10 mM	0.104 ml	0.522 ml	1.044 ml
  50 mM	0.021 ml	0.104 ml	0.209 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *