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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
- 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
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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 分子量 (g/mol)
