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。
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-actingangiotensin receptor-neprilysin (ARN)inhibitor for hypertension and heart failure[1][2][3]. Sacubitril/Valsartan ameliorates diabetic cardiomyopathy by inhibiting inflammation, oxidative stress andapoptosis[4]. |
IC50& Target | Angiotensin receptor-neprilysin[1] |
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)[4]. 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[4].
Apoptosis Analysis[4] 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[4] 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. |
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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[2].
Animal Model: | Adult 6- to 8-week-old male Sprague-Dawley rats (220-250 g body weight)[2] | 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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(104.39 mM) H2O : ≥ 50 mg/mL(52.19 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 1.0439 mL | 5.2193 mL | 10.4385 mL | 5 mM | 0.2088 mL | 1.0439 mL | 2.0877 mL | 10 mM | 0.1044 mL | 0.5219 mL | 1.0439 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: PBS Solubility: 100 mg/mL (104.39 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (2.61 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (2.61 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (2.61 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (2.61 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (2.61 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (2.61 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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