LCZ696

LCZ696 Struktur
936623-90-4
CAS-Nr.
936623-90-4
Englisch Name:
LCZ696
Synonyma:
Entresto;LZC696;Valsartan/sacubitril;LCZ696(Sacubitril/Valsartan);Sacubitril/Valsartan Trisodium Salt;Sacubitril valsartan sodium hydrate;LCZ696;LCA696;Secubitril;LCZ696;LCZ 696
CBNumber:
CB72715242
Summenformel:
C48H58N6O8
Molgewicht:
847.03
MOL-Datei:
936623-90-4.mol

LCZ696 Eigenschaften

storage temp. 
Store at -20°C
Löslichkeit
≥45.05 mg/mL in DMSO; ≥11.28 mg/mL in H2O; ≥28.5 mg/mL in EtOH
Aggregatzustand
solid
Farbe
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|

Sicherheit

LCZ696 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

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.

Handelsname

Entresto

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.

Einzelnachweise

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 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


LCZ696 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global( 369)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Zibo Wei Bin Import & Export Trade Co. Ltd.
+86-0533-2091136 +8613864437655
ziboweibinmaoyi@163.com China 100 58
ChemExpress
+86-021-58950125 +86-021-58950125;
info@chemexpress.com China 737 58
Sinoway Industrial co., ltd.
0592-5800732; +8613806035118
xie@china-sinoway.com China 988 58
Hangzhou Hyper Chemicals Limited
+86-0086-57187702781 +8613675893055
info@hyper-chem.com China 295 58
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
+86-18600796368 +86-18600796368
sales@sjar-tech.com China 444 58
Cangzhou Kangrui Pharma Tech Co. Ltd.,
+86-18632776803 +86-13833998158
cangzhoukangrui@126.com China 737 58
Capot Chemical Co.,Ltd.
+86-(0)57185586718 +86-13336195806
sales@capot.com China 29791 60
Nanjing Gold Pharmaceutical Technology Co. Ltd.
025-84209270 15906146951
CHINA 115 55
Beijing Cooperate Pharmaceutical Co.,Ltd
010-60279497
sales01@cooperate-pharm.com CHINA 1803 55
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512
info@tianfuchem.com China 21634 55

  • [(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
  • ,LCZ696 valsartan + sacubitril Sodium impurity 58
  • 936623-90-4
  • C49H60N6O8
  • C24H29N5O3C24H29NO552H2O3Na
  • 2C24H29N5O32C24H29NO55H2O6Na
  • C24H27N5Na2O3C24H28NNaO5xH2O
  • C48H55N6Na3O8
  • C48H54N6Na3O825H2O
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