产品属性:
产品名称 | 规格 | CAS号 | 型号 |
LCZ696 | 10mM (in 1mL DMSO) 5mg 25mg 100mg | 936623-90-4 | EY-Y0164342 |
Cas No.936623-90-4
别名 N/A
化学名 N/A
分子式 C48H54N6Na3O8.2.5H2O
分子量 956.99
溶解度 ≥ 45.05mg/mL in DMSO
储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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),
关键字: 936623-90-4;C48H54N6Na3O8.2.5H2O;LCZ696;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要从事免疫学、分子生物学和常规生化试剂等为一体的科研产品销售企业,公司自成立以来,秉承""全心全意服务于科研工作者""的企业理念,立足生物科技领域,运用生物技术和科研试剂,发展现代生物科技,为各类大中小医院及其它医疗机构、高等院校、科研院所、企事业单位提供优质的产品,服务生物科技领域的科学研究人员。
公司具有对普通货物、冷藏及冷冻仓库的存储、包装及运输能力。
公司将始终坚持信誉立业、以人为本、质量保证、诚信服务的宗旨,不断拼搏,开拓进取,与各界朋友携手共创美好未来。