价格:966
货号LCZ696
产品详情
产品详情
产品信息
产品名称 |
产品编号 |
规格 |
价格(元) |
LCZ696 | HR11784-5 | 5mg | 966 |
LCZ696 | HR11784-5.1 | 10mM(in1mLDMSO) | 1712 |
LCZ696 | HR11784-25 | 25mg | 2394 |
LCZ696 | HR11784-100 | 100mg | 5051 |
产品描述
LCZ696 is a first in class ARNi (angiotensin receptor neprilysin inhibitor) comprising anionic moieties of AR valsartan and the neprilysin inhibitor prodrug AHU377 (1:1 ratio) for heart failure and hypertension.
The angiotensin receptors are G-protein-coupled receptors. They mediate the cardiovascular and other effects of angiotensin II which is a bioactive peptide of the renin–angiotensin system. Neprilysin is a neutral endopeptidase that degrades endogenous vasoactive peptides such as natriuretic peptides. Inhibition of neprilysin increases the natriuretic peptides concentration that contributed to cardiac, vascular and renal protection. [1]
In Sprague-Dawley rats, oral administration of LCZ696 led to a dose-dependent rise in immunoreactivity of atrial natriuretic peptide resulting from neprilysin inhibition. In hypertensive double transgenic rats, LCZ696 caused a dose-dependent and sustained reduction in mean arterial pressure. A healthy participants, a randomized, double-blind, placebo-controlled study confirmed that LCZ696 provided concurrent neprilysin inhibition and AT1 receptor blockade. LCZ696 was safe and well tolerated in human. [2] [3]
References:
[1].McMurray JJ, Packer M, Desai AS et al. Angiotensin-neprilysin inhibition versus enalapril in heart failure. N Engl J Med. 2014 Sep 11;371(11):993-1004.
[2].Gu J, Noe A, Chandra P, Al-Fayoumi S 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.
[3].Langenickel TH, Dole WP. Angiotensin receptor-neprilysin inhibition with LCZ696: a novel approach for the treatment of heart failure, Drug Discov Today: Ther Strategies (2014),
产品特性
品目 | 描述 |
CAS | 936623-90-4 |
分子式 | C48H54N6Na3O8.2.5H2O |
分子量 | 956.99 |
溶解度 | ≥ 45.05mg/mL in DMSO |
储存 | Store at -20°C |
运输储存方法
按照产品包装上标识运输储存。
注意事项
1. 为了您的安全和健康,请穿实验服并戴一次性手套操作。
2. 本产品仅作科研用途!