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Sacubitril hemicalcium salt

Catalog No. T4200   CAS 1369773-39-6
Synonyms: AHU-377 (hemicalcium salt), AHU377 calcium salt

Sacubitril hemicalcium salt (AHU377 calcium salt) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril hemicalcium salt is a component of the heart failure medicine LCZ696. Sacubitril hemicalcium salt is a prodrug of LBQ657, which is an inhibitor of the zinc metallopeptidase neprilysin. Neprilysin degrades a variety of vasoactive peptides such as atrial and brain natriuretic peptide, bradykinin, adrenomedullin, and endothelin-1. Inhibition of neprilysin leads to an increased level of these peptides and, thus, antihypertensive effects. Formulations containing AHU377 in combination with the angiotensin II receptor antagonist valsartan are used to treat hypertension and heart failure.

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Sacubitril hemicalcium salt Chemical Structure
Sacubitril hemicalcium salt, CAS 1369773-39-6
Pack Size Availability Price/USD Quantity
2 mg In stock $ 33.00
5 mg In stock $ 48.00
10 mg In stock $ 58.00
25 mg In stock $ 86.00
50 mg In stock $ 108.00
100 mg In stock $ 157.00
200 mg In stock $ 217.00
1 mL * 10 mM (in DMSO) In stock $ 58.00
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Purity: 99.28%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Sacubitril hemicalcium salt (AHU377 calcium salt) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril hemicalcium salt is a component of the heart failure medicine LCZ696. Sacubitril hemicalcium salt is a prodrug of LBQ657, which is an inhibitor of the zinc metallopeptidase neprilysin. Neprilysin degrades a variety of vasoactive peptides such as atrial and brain natriuretic peptide, bradykinin, adrenomedullin, and endothelin-1. Inhibition of neprilysin leads to an increased level of these peptides and, thus, antihypertensive effects. Formulations containing AHU377 in combination with the angiotensin II receptor antagonist valsartan are used to treat hypertension and heart failure.
Targets&IC50 NEP:5 nM
In vitro AHU377 is converted by enzymatic cleavage of the ethyl ester into the active neprilysin inhibiting metabolite LBQ657. The inactive NEPi precursor, AHU377, does not inhibit collagen accumulation in fibroblasts nor cardiac myocyte hypertrophy. In cardiac fibroblasts, the active NEPi LBQ657 had no discernible effects. In contrast, LBQ657 modestly inhibits cardiac myocyte hypertrophy.
In vivo In humans, AHU377 (tmax 0.5-1.1 h) are absorbed quickly. AHU377 is converted rapidly into LBQ657 with its tmax being reached in 1.9-3.5 h. Mean t1/2 values for the biologically active LBQ657 is 9.9-11.1 h.In vehicle-treated dogs, ANF increases urinary sodium excretion from 17.3±3.6 to 199.5±18.4 pequivkglmin. This effect is potentiated significantly in animals which receive AHU377.
Synonyms AHU-377 (hemicalcium salt), AHU377 calcium salt
Molecular Weight 861.06
Formula C48H56CaN2O10
CAS No. 1369773-39-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 54 mg/mL

TargetMolReferences and Literature

1. Schiering N,et al. Structure of neprilysin in complex with the active metabolite of sacubitril.Sci Rep. 2016 Jun 15;6:27909.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library FDA-Approved Drug Library Anti-Hypertension Compound Library Approved Drug Library Anti-Aging Compound Library Anti-Cardiovascular Disease Compound Library Drug Repurposing Compound Library Bioactive Compound Library FDA-Approved & Pharmacopeia Drug Library Bioactive Compounds Library Max

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LHW090-A7 Sacubitrilat Phosphoramidon Disodium NEP-IN-1 Racecadotril Sacubitril/Valsartan Sacubitril Thiorphan

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Keywords

Sacubitril hemicalcium salt 1369773-39-6 Metabolism Neprilysin Cluster of differentiation 10 AHU-377 AHU377 NEP inhibit CD10 Sacubitril hemicalcium Sacubitril AHU-377 (hemicalcium salt) Neutral endopeptidase AHU 377 AHU377 calcium salt AHU-377 hemicalcium AHU377 calcium Inhibitor inhibitor

 

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