AHU-377 (heMicalciu...

AHU-377 (heMicalciuM salt)

AHU-377 (heMicalciuM salt)

Min.Order / FOB Price:Get Latest Price

100 Gram

FOB Price: USD 1.0000

  • Min.Order :100 Gram
  • Purity: ≥98.0%
  • Payment Terms : L/C

Keywords

1369773-39-6 AHU-377 (heMicalciuM salt) AHU-377 (heMicalciuM salt);(alphaR,gammaS)-gamma-[(3-Carboxy-1-oxopropyl)amino]-alpha-methyl-[1,1'-biphenyl]-4-pentanoic acid 4-ethyl ester calcium salt (2:1);(2S,4R)-5-(Biphenyl-4-yl)-4-[(3-carboxypr

Quick Details

  • Appearance:white powder
  • Application:LCZ696 intermediates; Pharmaceutical Intermediates. Pharmaceutical intermediates. Impurity reference substance; LCZ696 intermediates
  • PackAge:100g,500g,1kg,25kg/drum
  • ProductionCapacity:1000|Gram|Week
  • Storage:Dry seal
  • Transportation:shipping

Superiority:

We are specialized in custom synthesis, chemical/pharmaceutical/ pesticides outsourcing and contract research.
 
 
 
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Our research team of scientists consists of western-trained Ph.D.s with experience and capabilities in drug R&D methodologies and medicinal chemistry.

 

Details:

AHU-377 hemicalcium salt is a potent neprilysin inhibitor with IC50 of 5.0 nM; a component of LCZ696.
IC50 Value: 5.0 nM
Target: neprilysin
in vitro:
in vivo: LCZ696 is a novel single molecule comprising molecular moieties of valsartan and NEP inhibitor prodrug AHU377 (1:1 ratio). 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.

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