| 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。 |