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LCZ696

Valsartan & sacubitril,LCZ 696,LCZ-696

LCZ696是首个2型血管紧张素受体（AT II）和脑啡肽酶（neprilysin）双重抑制剂，由Valsartan和NEP抑制剂前提药物AHU377(1:1)组成。

目录号
EY1658
EY1658
EY1658
EY1658
EY1658
纯度
99.55%
99.55%
99.55%
99.55%
99.55%
规格
1 mg
5 mg
10 mg
25 mg
50 mg
原价
456
880.00
1200.00
2200.00
3780.00
售价
456
880.00
1200.00
2200.00
3780.00
库存
现货
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
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  • 生物活性

    LCZ696, consisting of valsartan and sacubitril in 1:1 molar ratio, is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. Phase 3.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    ~60 mg/kgp.o.

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Gu J, et al. J Clin Pharmacol. 2010, 50(4), 401-414.

    分子式
    C48H55N6O8(-3)    		 分子量
    843.99    		 CAS号
    936623-90-4    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    30 mg/mL    		 Water
    100 mg/mL    		 Ethanol
    8 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT01569815 Mild and Moderate Renal Impairment Drug: LCZ696 Novartis Pharmaceuticals|Novartis Phase 1 2009-02-01 2015-09-25
    NCT01922089 Heart Failure With Reduced Ejection Fraction Drug: LCZ696 Novartis Pharmaceuticals|Novartis Phase 2 2013-11-01 2015-09-16
    NCT02690974 Hearth Failure With Reduced Ejection Fraction (HFrEF) Drug: LCZ696 (sacubitril/valsartan) Novartis Pharmaceuticals|Novartis Phase 4 2016-03-09 2017-02-28
    NCT02661217 Heart Failure With Reduced Ejection Fraction (HFrEF) Drug: LCZ696 Novartis Pharmaceuticals|Novartis Phase 4 2016-02-12 2017-03-07
    NCT00913653 Heart Failure Drug: LCZ696 Novartis Pharmaceuticals|Novartis Phase 2 2009-05-01 2016-11-16
    NCT01601470 Mild to Moderate Hypertension Drug: LCZ696|Drug: Sildenafil Novartis Pharmaceuticals|Novartis Phase 2 2012-09-01 2015-10-06
    NCT01681576 Salt-sensitive Hypertension Drug: Valsartan|Drug: LCZ696 Novartis Pharmaceuticals|Novartis Phase 2 2012-08-01 2015-10-12
    NCT01785472 Essential Hypertension Drug: LCZ696|Drug: Olmesartan|Drug: Placebo of LCZ696|Drug: Placebo of Olmesartan Novartis Pharmaceuticals|Novartis Phase 3 2013-04-01 2016-11-08
    NCT01646671 Severe Hypertension Drug: LCZ696|Drug: LCZ696|Drug: LCZ696 Novartis Pharmaceuticals|Novartis Phase 3 2012-07-01 2015-10-02
    NCT02226120 Chronic Heart Failure With Reduced Ejection Fraction Drug: LCZ696 Novartis Pharmaceuticals|Novartis Phase 3 2014-10-16 2017-03-07
    NCT01569828 Pharmacokinetics|Renal Impaired|Healthy Volunteer Drug: LCZ696A|Drug: LCZ696A Novartis Pharmaceuticals|Novartis Phase 2 2009-03-01 2015-08-27
    NCT01593787 Hypertension With Renal Dysfunction Drug: LCZ696 Novartis Pharmaceuticals|Novartis Phase 3 2012-05-01 2015-08-07
    NCT01631864 Hypertension|Concurrent Obesity Drug: LCZ696|Drug: amlodipine|Drug: Placebo Novartis Pharmaceuticals|Novartis Phase 2 2012-10-01 2015-07-11
    NCT02816736 Heart Failure Drug: LCZ696|Drug: valsartan|Drug: LCZ696 placebo|Drug: valsartan placebo Duke University|National Heart, Lung, and Blood Institute (NHLBI) Phase 4 2017-03-02 2017-03-08
    NCT02916160 Chronic Heart Failure|Sleep Apnea Syndrome Drug: SACUBITRIL - VALSARTAN (formerly LCZ696, ENTRESTO) University Hospital, Montpellier 2016-09-01 2016-09-23
    NCT01615198 Essential Hypertension Drug: Olmesartan|Drug: Placebo|Drug: LCZ696 Novartis Pharmaceuticals|Novartis Phase 3 2012-08-01 2015-10-01
    NCT01621633 Hepatic Impairment Drug: LCZ696 Novartis Pharmaceuticals|Novartis Phase 2 2012-09-01 2015-07-11
    NCT01599104 Essential Hypertension Drug: LCZ696|Drug: Olmesartan|Drug: Placebo Novartis Pharmaceuticals|Novartis Phase 3 2012-06-01 2015-09-25
    NCT01353508 Hypertension Drug: LCZ696|Drug: Valsartan Novartis Pharmaceuticals|Novartis Phase 2 2011-03-01 2015-10-20
    NCT01920711 Heart Failure With Preserved Ejection Fraction Drug: LCZ696|Drug: Valsartan Novartis Pharmaceuticals|Novartis Phase 3 2014-07-18 2017-03-07
    NCT01035255 Heart Failure With Reduced Ejection Fraction Drug: LCZ696 200 mg BID|Drug: Enalapril 10 mg BID Novartis Pharmaceuticals|Novartis Phase 3 2009-12-01 2016-07-13

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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