| Name | Sacubitrilat |
| Description | Sacubitrilat (LBQ-657) (LBQ657) is an effective inhibitor of active neprilysin (NEP). |
| In vitro | Sacubitrilat is bound to the active site of NEP by an intricate network of interactions that involves all functional groups of the compound giving rise to the high inhibitory potency of 5?nM [1]. |
| In vivo | Pharmacokinetics of Sacubitril, Sacubitrilat, and valsartan following the administration of single oral doses of LCZ696 400 or 1200 mg under fasting conditions are summarized. The mean plasma concentrations of Sacubitril increases rapidly with a median Tmax of 0.52 h for the 400 mg dose and 1.05 h for the 1200 mg dose, followed by Sacubitrilat, with the corresponding Tmax values of 2.07 and 3.05 h, respectively. The median Tmax for valsartan is 2.07 h for both the LCZ696 400 mg and 1200 mg doses. The Cmax of Sacubitrilat shows a dose-proportional increase, while the Cmax of Sacubitril and Valsartan shows less than proportional increases between the doses [2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (10.43 mM), Sonication is recommended. DMSO : 100 mg/mL (260.8 mM), Sonication is recommended.
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| Keywords | Sacubitrilat | Neutral endopeptidase | Neprilysin | NEP | LBQ657 | LBQ 657 | Inhibitor | inhibit | Desethyl Sacubitril | Cluster of differentiation 10 | CD10 |
| Inhibitors Related | LHW090-A7 | Sacubitril/Valsartan | Sacubitril sodium | Candoxatril | Omapatrilat | Racecadotril | Sacubitril | NEP-IN-1 | Phenylalanylalanine | Sacubitril hemicalcium salt | Thiorphan | Dexecadotril |
| Related Compound Libraries | Bioactive Compound Library | ReFRAME Related Library | Inhibitor Library | NO PAINS Compound Library | Metabolism Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library | Human Metabolite Library |