| Name | Sacubitril |
| Description | Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM and is a component of the heart failure medicine LCZ696. |
| In vitro | LCZ696 is a single molecule that is comprised of molecular moieties of valsartan, an ARB, and Sacubitril, a neprilysin inhibitor (1:1 ratio). Sacubitril is converted by enzymatic cleavage of the ethyl ester into the active neprilysin inhibiting metabolite LBQ657[2]. The inactive NEPi precursor, Sacubitril, 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[3]. |
| In vivo | In humans, Sacubitril (tmax0.5-1.1 h) are absorbed quickly. Sacubitril is converted rapidly into LBQ657 with its tmaxbeing reached in 1.9-3.5 h. Mean t1/2values for the biologically active LBQ657 is 9.9-11.1 h[2].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 Sacubitril. Urinary volume is also potentiated in animals which receive an iv administration of Sacubitril[1]. |
| Storage | Pure form: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 27.5 mg/mL (66.83 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.86 mM), Sonication is recommended.
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| Keywords | Sacubitril | neutral endopeptidase (NEP) | Neutral endopeptidase | Neprilysin | NEP | natriuretic peptide | Inhibitor | inhibit | heart failure | COVID-19 | Cluster of differentiation 10 | CD10 | antihypertensive |
| Inhibitors Related | LHW090-A7 | Sacubitril/Valsartan | Sacubitril sodium | Candoxatril | Omapatrilat | Racecadotril | NEP-IN-1 | Phenylalanylalanine | Sacubitril hemicalcium salt | Thiorphan | TD-0212 TFA | Sacubitrilat |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Pediatric Drug Library | EMA Approved Drug Library | Drug Repurposing Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Cardiovascular Disease Compound Library | FDA-Approved Drug Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library | Anti-Hypertension Compound Library |
United States
