Sacubitril hemicalcium salt

SKU: orb1303069

Description

Sacubitril hemicalcium salt (AHU377) is a potent prodrug neprilysin (NEP) inhibitor (IC50 = 5 nM) metabolized to active LBQ657. As a key component of LCZ696 (valsartan/sacubitril), it is widely used in cardiovascular research, particularly in studies of hypertension and heart failure, to investigate NEP inhibition's effects on natriuretic peptides in vitro and in animal models.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1369773-39-6
• MW: 861.06
• Purity: 99.93% (May vary between batches)
• Formula: C₄₈H₅₆CaN₂O₁₀
• SMILES: [Ca++].CCOC(=O)[C@H](C)C[C@@H](Cc1ccc(cc1)-c1ccccc1)NC(=O)CCC([O-])=O.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:5 mg/mL (5.81 mM);DMSO:60 mg/mL (69.68 mM)

Bioactivity

• Target IC50:
  NEP:5 nM
• 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.
• 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.

Storage & Handling

• Storage: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Neprilysin, NEP, neutral endopeptidase (NEP), Neutral endopeptidase, inhibit, Inhibitor, AHU377, AHU-377, AHU-377 (hemicalcium salt), AHU377 calcium salt, AHU377 calcium, AHU-377 hemicalcium, AHU 377, Cluster of differentiation 10, CD10, Sacubitril hemicalcium, Sacubitril hemicalcium salt, Sacubitril

Compound Identifiers

PubChem CID

92045585