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 |
| 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. |
| 分子式 | C48H58N6O8 |
| 分子量 | 847.03 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存条件 | Powder -20°C 3 years |
| 溶解性数据 | DMSO : ≥ 35 mg/mL (100.07 mM) 0.1 M NaOH : 33.33 mg/mL (95.29 mM; ultrasonic and adjust pH to 9 with NaOH) |
| 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. |
| 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. |
| 文献 | •Oxid Med Cell Longev. 2020 Sep 17;2020:9815039. •Front Pharmacol. 2021 Sep 2;12:724147. •Exp Biol Med (Maywood). 2019 Sep;244(12):1028-1039. |
| 纯度及产品资料 | 98% |
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