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LCZ696

In stock
Catalog No.
B4815
A first in class ARNi (angiotensin receptor neprilysin inhibitor)
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$240.00
In stock
5mg
$124.00
In stock
25mg
$334.00
In stock
100mg
$698.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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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:
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.
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.
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),

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt956.99
Cas No.936623-90-4
FormulaC48H54N6Na3O8.2.5H2O
Solubility≥45.05mg/mL in DMSO
SDFDownload SDF
Canonical SMILESCCCCC(N([[email protected]@](C([O-])=O)([H])C(C)C)CC1=CC=C(C2=CC=CC=C2C3=N[N-]N=N3)C=C1)=O.CCOC([[email protected]](C[[email protected]@](/N=C([O-])/CCC([O-])=O)([H])CC4=CC=C(C5=CC=CC=C5)C=C4)([H])C)=O.[3Na+].[2.5H2O]
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Chemical structure

LCZ696