Sacubitril

SKU: orb1302745

Description

Sacubitril

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 149709-62-6
• MW: 411.49
• Purity: 98.71% (May vary between batches)
• Formula: C₂₄H₂₉NO₅
• SMILES: CCOC(=O)[C@H](C)C[C@@H](Cc1ccc(cc1)-c1ccccc1)NC(=O)CCC(O)=O
• Target: Neprilysin
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.86 mM);DMSO:27.5 mg/mL (66.83 mM)

Bioactivity

• Target IC50:
  NEP:5 nM
• 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.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.
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• 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. 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Sacubitril, NEP, Neprilysin, Neutral endopeptidase, neutral endopeptidase (NEP), natriuretic peptide, inhibit, Inhibitor, heart failure, antihypertensive, AHU-377, AHU377, AHU 377, COVID-19, Cluster of differentiation 10, CD10

Compound Identifiers

PubChem CID

9811834