Sacubitril/Valsartan 沙库必曲/缬沙坦; LCZ696,99.99%

产品编号:Bellancom-18204A| CAS NO:936623-90-4| 分子式:C48H55N6Na3O8.2.5H2O| 分子量:957.99

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-18204A
1100.00 杭州 北京(现货)
Bellancom-18204A
1550.00 杭州 北京(现货)
Bellancom-18204A
3980.00 杭州 北京(现货)

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Sacubitril/Valsartan 沙库必曲/缬沙坦; LCZ696

产品介绍 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-acting angiotensin receptor-neprilysin (ARN) inhibitor for hypertension and heart failure. Sacubitril/Valsartan ameliorates diabetic cardiomyopathy by inhibiting inflammation, oxidative stress and apoptosis[4].

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)[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].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
性状Solid
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
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 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 西域 网站选购。
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)

参考文献

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