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ChemicalBook > Product Catalog >Biochemical Engineering >Inhibitors >Endocrinology & Hormones >RAAS inhibitors >LCZ696

LCZ696

LCZ696 Structure
CAS No.
936623-90-4
Chemical Name:
LCZ696
Synonyms
Entresto;LZC696;Valsartan/sacubitril;LCZ696(Sacubitril/Valsartan);Sacubitril/Valsartan Trisodium Salt;Sacubitril valsartan sodium hydrate;LCZ696;LCA696;Secubitril;LCZ696;LCZ 696
CBNumber:
CB72715242
Molecular Formula:
C48H58N6O8
Molecular Weight:
847.03
MOL File:
936623-90-4.mol
MSDS File:
SDS
Modify Date:
2024/9/19 18:11:18
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LCZ696 Properties

storage temp. Store at -20°C
solubility ≥45.05 mg/mL in DMSO; ≥11.28 mg/mL in H2O; ≥28.5 mg/mL in EtOH
form solid
color White to light yellow
InChIKey XTKIDERFOUYBDE-NOFROVMTNA-N
SMILES C(C1C=CC(C2C=CC=CC=2C2=NN=NN2)=CC=1)N(C(=O)CCCC)[C@H](C(=O)O)C(C)C.C(C1C=CC(C2C=CC=CC=2)=CC=1)[C@@H](NC(=O)CCC(=O)O)C[C@@H](C)C(=O)OCC |&1:25,45,55,r|

SAFETY

Risk and Safety Statements

Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H302+H312-H315+H320

LCZ696 Chemical Properties,Uses,Production

Description

LCZ696 is a dual angiotensin II receptor antagonist and neprilysin inhibitor that is a combination of the nonpeptide angiotensin II receptor antagonist valsartan and AHU377 , a prodrug of LBQ657 , which is an inhibitor of the zinc metallopeptidase neprilysin., LCZ696 (2-60 mg/kg) induces a dose-dependent decrease in mean arterial pressure in rats expressing human renin and angiotensinogen, a double-transgenic model for angiotensin II-dependent hypertension. Formulations containing LCZ696 are under clinical investigation for the treatment of mild to moderate hypertension and chronic heart failure.

Mechanism of action

LCZ696 is a molecule that combines the moieties of valsartan and sacubitril (the neprilysin inhibitor) in a single substance. By inhibiting neprilysin, the degradation of natriuretic peptides, bradykinin, and other peptides is slowed. Hence, high circulating levels of natriuretic peptides enhance diuresis , natriuresis, myocardial relaxation, and anti-remodelling, on top of the ARB effects of valsartan.

Clinical Use

LCZ696 (Novartis Pharmaceuticals), a first-in-class inhibitor of dualacting angiotensin-2 type-I receptor and neprilysin inhibitors, was developed as a molecule composed of molecular moieties of valsartan and neprilysin inhibitor prodrug AHU377 in a 1:1 ratio. Several phase 2 randomised clinical trials have been done or are underway in patients with hypertension. In a proof-of-concept randomised trial, LCZ696 was compared with valsartan in 1328 patients with mild-to-moderate hypertension, and provided fully additive reduction of blood pressure. No cases of angio-oedema were reported in the 8 week treatment period. This tolerance should be confirmed, particularly in black patients, for whom omapatrilat resulted in a higher occurrence of angio-oedema than in white patients. Indeed, in the proof-of-concept trial only about 8% of patients were black.

References

1. McMurray, John J. V. et al. “Angiotensin-neprilysin inhibition versus enalapril in heart failure.” The New England journal of medicine 371 11 (2014):  993-1004. DOI: 10.1056/NEJMoa1409077
2. Gu, Jessie et al. “Pharmacokinetics and Pharmacodynamics of LCZ696, a Novel Dual‐Acting Angiotensin Receptor—Neprilysin Inhibitor (ARNi).” The Journal of Clinical Pharmacology 50 (2010): n. pag. DOI: 10.1177/0091270009343932
3. Langenickel, T.H., & Dole, W.P. (2012). Angiotensin receptor-neprilysin inhibition with LCZ696: a novel approach for the treatment of heart failure. Drug Discovery Today: Therapeutic Strategies, 9. DOI: 10.1016/J.DDSTR.2013.11.002
4. Suematsu, Yasunori et al. “LCZ696, an angiotensin receptor–neprilysin inhibitor, improves cardiac function with the attenuation of fibrosis in heart failure with reduced ejection fraction in streptozotocin‐induced diabetic mice.” European Journal of Heart Failure 18 (2016): n. pag. DOI: 10.1002/ejhf.474

LCZ696 Preparation Products And Raw materials

Raw materials

Preparation Products

LCZ696 Suppliers

Global( 361)Suppliers
Supplier Tel Country ProdList Advantage Inquiry
Bulat Pharmaceutical Pvt Ltd +91-8448085659 +91-8448085660 Haryana, India 123 58 Inquiry
Viruj Pharmaceuticals Pvt Ltd +91-9441591589 +91-9441591589 Hyderabad, India 33 58 Inquiry
Shree HariKrishna Pharmaceuticals +91-9925611910 +91-9925611910 Gujarat, India 16 58 Inquiry
Exemed Pharmaceuticals (Oneiro Chemicals Pvt Ltd) +91-9687684674 +91-9099061028 Gujarat, India 30 58 Inquiry
Blue Jet Healthcare Ltd +91-02222071691 +91-9082861262 Mumbai, India 86 58 Inquiry
LUPIN LTD +91 124 4885000 / +91 124 3325000 New Delhi, India 191 58 Inquiry
CLEARSYNTH LABS LTD. +91-22-45045900 Hyderabad, India 6351 58 Inquiry
Pharmaffiliates Analytics and Synthetics P. Ltd +91-172-5066494 Haryana, India 6773 58 Inquiry
SynZeal Research Pvt Ltd +1 226-802-2078 Gujarat, India 6522 58 Inquiry
Bulat Pharmaceutical Private Limited 08048372574Ext 902 Haryana, India 37 58 Inquiry
Supplier Advantage
Bulat Pharmaceutical Pvt Ltd 58
Viruj Pharmaceuticals Pvt Ltd 58
Shree HariKrishna Pharmaceuticals 58
Exemed Pharmaceuticals (Oneiro Chemicals Pvt Ltd) 58
Blue Jet Healthcare Ltd 58
LUPIN LTD 58
CLEARSYNTH LABS LTD. 58
Pharmaffiliates Analytics and Synthetics P. Ltd 58
SynZeal Research Pvt Ltd 58
Bulat Pharmaceutical Private Limited 58

LCZ696 Spectrum

LCZ696(936623-90-4)1HNMR

936623-90-4(LCZ696)Related Search:

(R,E)-5-([1,1'-biphenyl]-4-yl)-4-((tert-butoxycarbonyl)aMino)-2-Methylpent-2-enoic acid Ethyl (2R,4S)-4-([1,1'-biphenyl]-4-ylmethyl)-2-methyl-4-(2,5-dioxopyrrolidin-1-yl)butanoate (2R,4S)-5-([1,1'-biphenyl]-4-yl)-4-aMino-2-Methylpentanoic acid hydrochloride (2S,4R)-5-(Biphenyl-4-yl)-4-[(tert-butoxycarbonyl)amino]-2-methylpentanoic acid (2R,4R)-5-(Biphenyl-4-yl)-4-[(tert-butoxycarbonyl)amino]-2-methylpentanoic acid
AHU-377 sacubitril (R,E)-ethyl 5-([1,1'-biphenyl]-4-yl)-4-((tert-butoxycarbonyl)aMino)-2-Methylpent-2-enoate (2R,4S)-4-([1,1'-Biphenyl]-4-ylmethyl)-4-(4-ethoxy-4-oxobutanamido)-2-methylbutanoic acid AHU-377 (heMicalciuM salt)
(2R,4S)-ethyl 5-([1,1'-biphenyl]-4-yl)-4-((tert-butoxycarbonyl)aMino)-2-Methylpentanoate (2R,4S)-5-([1,1'-biphenyl]-4-yl)-4-((tert-butoxycarbonyl)aMino)-2-Methylpentanoic acid (2R,4S)-ethyl 5-([1,1'-biphenyl]-4-yl)-4-aMino-2-Methylpentanoate LCZ696 interMediate ((R)-2-biphenyl-4-yl-1-forMylethyl)carbaMic acid t-butyl ester
(2R,4S)-4-([1,1'-Biphenyl]-4-ylmethyl)-2-methyl-4-(2,5-dioxopyrrolidin-1-yl)butanoic acid (S)-5-[(Biphenyl-4-yl)carbonyl]pyrrolidin-2-one Valsartan
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[(C24H29N5O3).(C24H29NO5).2.5(H2O).3Na] LCZ696 ENTRESTO TM LCZ696 Entresto 4-[[(2S,4R)-5-ethoxy-4-methyl-5-oxo-1-(4-phenylphenyl)pentan-2-yl]amino]-4-oxobutanoate Sacubitril mixture with Valsartan Cocrystal of Sacubitril and Valsartan (S)-2-(N-((2'-(1H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)hexanamido)-3-methylbutanoic acid lcz696/Valsartan/sacubitril Sacubitril-Valsartan complex 3-(1-Biphenyl-4-ylMethyl-3-ethoxycarbonyl-1-butylcarbaMoyl)propionate-3'-Methyl-2'-(pentanoyl(2'-(tetrazol-5-ylate)biphenyl-4'-ylMethyl)aMino)butyrate LCZ696 LCZ696 interMediate N-(1-oxopentyl)-N-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-L-valine, compd. with α-ethyl (αR,γS)-γ-[(3-carboxy-1-oxopropyl)amino]-α-methyl[1,1'-biphenyl]-4-pentanoate, sodium salt, hydrate (2) Valsartan-sacubitril(LCZ696) sodium (S)-5-(4'-((N-(1-carboxylato-2-methylpropyl)pentanamido)methyl)-[1,1'-biphenyl]-2-yl)tetrazol-1-ide 4-(((2S,4R)-1-([1,1'-biphenyl]-4-yl)-5-ethoxy-4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoate LCZ696 (936623-90-4) Valsartan/Sacubitril (1:1) Entresto,Valsartan/sacubitril LCZ696 (Shakubi Qusarsartan) LCZ696;LCZ 696 Entresto (sacubitril/valsartan) LCZ696 Valsartan-Sacubitril sodium LCZ696 (Valsartan) LCA696 Sacubitril Valsartan (LCZ696) Entresto（LCZ696） Sacubatro valsartan LCZ696 USP/EP/BP Secubitril Radix isatidis polysaccharides Sacubatril/Valsartan Entresto LZC696 Valsartan/sacubitril LCZ696(Sacubitril/Valsartan) Sacubitril/Valsartan Trisodium Salt Sacubitril valsartan sodium hydrate Sand library will be LCZ696 (Valsarta + Sacubitril) 1H-Isoindole-1,3(2H)-dione,2-[2-(3,4-dihydro-2,2,4-trimethyl-1(2H)-quinolinyl)-5-oxoethyl]- Sacubitril-Valsartan trisodium salt hydrate Sacubitril Valsartan cocrystal (LCZ696) Sacubitril-Valsartan Trisodium Salt 2.5hydrate Sacubatrava valsartan Sakubitrexovalsartan Sacubitril/Valsartan LCZ API Sacubitril Valsatran Co Crystal In-House Sacubitril-Valsartan Trisodium Salt 2.5H2O Sacubitril Valsartan trisodium hydrate LCZ696（valsartan + sacubitril）Sodium impurity 58 2.5 Hydrate 936623-90-4 C49H60N6O8 C24H29N5O3C24H29NO552H2O3Na 2C24H29N5O32C24H29NO55H2O6Na C24H27N5Na2O3C24H28NNaO5xH2O C48H55N6Na3O8 C48H54N6Na3O825H2O Cardiovascular Series