AHU-377 hemicalcium salt - CAS 1369773-39-6
Not Intended for Therapeutic Use. For research use only.
Category:
Inhibitor
Product Name:
AHU-377 hemicalcium salt
Catalog Number:
1369773-39-6
Synonyms:
Sacubitril hemicalcium salt; AHU377 hemicalcium salt; AHU 377 hemicalcium salt
CAS Number:
1369773-39-6
Description:
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.
Molecular Weight:
410.48
Molecular Formula:
C24H28NO5-
COA:
Inquire
MSDS:
Inquire
Targets:
Neprilysin
Chemical Structure
CAS 1369773-39-6 AHU-377 hemicalcium salt

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Reference Reading


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Novozhilov YV1, Dorogov MV1, Blumina MV1, Smirnov AV1, Krasavin M2. Chem Cent J. 2015 Feb 13;9:7. doi: 10.1186/s13065-015-0082-7. eCollection 2015.
BACKGROUND: If literature protocols are followed, conversion of an advanced ketal ester intermediate (available in kilogram quantities via a published Paal-Knorr synthesis) to cholesterol-lowering drug atorvastatin calcium is hampered by several process issues, particularly at the final stage where the hemi-calcium salt is obtained.
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Zhang Y1, McBride DW Jr, Hamill OP. J Physiol. 1998 May 1;508 ( Pt 3):763-76.
1. The ion selectivity of a membrane ion conductance that is inactivated by extracellular calcium (Ca2+o) in Xenopus oocytes has been studied using the voltage-clamp technique. 2. The reversal potential of the Ca2+o-sensitive current (Ic) was measured using voltage ramps (-80 to +40 mV) as a function of the external concentration (12-240 mM) of NaCl or KCl. The direction and amplitude of the shifts in reversal potentials are consistent with permeability ratios of 1:0.99:0.24 for K+:Na+:Cl-. 3. Current-voltage (I-V ) relations of Ic, determined during either voltage ramps of 0.5 s duration or at steady state, displayed pronounced rectification at both hyperpolarized and depolarized potentials. However, instantaneous I-V relations showed less rectification and could be fitted by the constant field equation assuming the above K+:Na+:Cl- permeability ratios. 4. Ion substitution experiments indicated that relatively large organic monovalent cations and anions are permeant through Ic channels with the permeability ratios K+:NMDG+:TEA+:TPA+:TBA+:Gluc- = 1:0.