[Chemical Name]: |
Valsartan/sacubitril; LCZ-696; LCZ 696
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[Synonyms ]: |
Entresto; L-Valine, N-(1-oxopentyl)-N-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-, compd. with α-ethyl (αR,γS)-γ-[(3-carboxy-1-oxopropyl)amino]-α-methyl[1,1'-biphenyl]-4-pentanoate, sodium salt, hydrate (2:2:6:5); trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl)propionate-(S)-3-methyl-2-(pentanoyl{2”-(tetrazol-5-ylate)biphenyl-4-ylmethyl}amino)butyrate] hemipentahydrate; trisodium 3-((1S,3R)-1-(biphenyl-4-ylmethyl)-3-(ethoxycarbonyl)butylcarbamoyl)propionate (S)-3-methyl-2-(pentanoyl-(2-(tetrazol-1-at-5-yl)biphenyl-4'-ylmethyl)amino)butyrate hemipentahydrate
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[CAS No.]: |
936623-90-4
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[Structure Formula]: |
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[Molecular Formula]: |
C48H55N6Na3O8 / C48H55N6O8(-3)
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[Molecular Weight]: |
843.99
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[Solubility]: |
in DMSO > 10 mM
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[Purity ( Assay ) ]: |
99.0% min
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[Biological activity ]: |
LCZ696 is a first-in-class dual inhibitor of the angiotensin II receptor(AT II receptor) and neprilysin; a novel single molecule comprising molecular moieties of valsartan and NEP inhibitor prodrug AHU377 (1:1 ratio).
IC50 value:
Target: AT II receptor; neprilysin
Oral administration of LCZ696 caused dose-dependent increases in atrial natriuretic peptide immunoreactivity (due to NEP inhibition) in Sprague-Dawley rats and provided sustained, dose-dependent blood pressure reductions in hypertensive double-transgenic rats. In healthy participants, a randomized, double-blind, placebo-controlled study (n = 80) of single-dose (200-1200 mg) and multiple-dose (50-900 mg once daily for 14 days) oral administration of LCZ696 showed that peak plasma concentrations were reached rapidly for valsartan (1.6-4.9 hours), AHU377 (0.5-1.1 hours), and its active moiety, LBQ657 (1.8-3.5 hours) . LCZ696 is superior to valsartan alone in reducing blood pressure. Preliminary results from a Phase II trial showed that LCZ696 reduced NT-proBNP to a greater extent than valsartan alone, and in addition LCZ696 had beneficial effects on symptoms . |
[Usage/Application]: |
LCZ696 is used for the treatment of heart failure , LCZ696 is believed to be able to reduce the pressure of heart failure, and promote heart muscle ability
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[Packing]: |
In small aluminum foil bag or 1kg-10kg Tin
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