1. Metabolic Enzyme/Protease
  2. Neprilysin
  3. Sacubitril

Sacubitril (Synonyms: AHU-377)

Cat. No.: HY-15407 Purity: 99.71% ee.: 100.00%
Handling Instructions

Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril (AHU-377) is a component of the heart failure medicine LCZ696.

For research use only. We do not sell to patients.

Sacubitril Chemical Structure

Sacubitril Chemical Structure

CAS No. : 149709-62-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
Estimated Time of Arrival: December 31
10 mg USD 96 In-stock
Estimated Time of Arrival: December 31
50 mg USD 180 In-stock
Estimated Time of Arrival: December 31
100 mg USD 300 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Description

Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril (AHU-377) is a component of the heart failure medicine LCZ696.

IC50 & Target

IC50: 5 nM (NEP)[1]

In Vitro

Sacubitril (AHU-377) is a single molecule that is comprised of molecular moieties of valsartan, an ARB, and Sacubitril (AHU-377), a neprilysin inhibitor (1:1 ratio). Sacubitril (AHU-377) is converted by enzymatic cleavage of the ethyl ester into the active neprilysin inhibiting metabolite LBQ657[2]. The inactive NEPi precursor, Sacubitril (AHU-377), 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 (AHU-377) (tmax 0.5-1.1 h) are absorbed quickly. Sacubitril (AHU-377) 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[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 (AHU-377). Urinary volume is also potentiated in animals which receive an iv administration of Sacubitril (AHU-377)[1].

Clinical Trial
Molecular Weight

411.49

Formula

C₂₄H₂₉NO₅

CAS No.

149709-62-6

SMILES

O=C(CCC(O)=O)N[[email protected]](CC1=CC=C(C2=CC=CC=C2)C=C1)C[[email protected]@H](C)C(OCC)=O

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (243.02 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4302 mL 12.1510 mL 24.3019 mL
5 mM 0.4860 mL 2.4302 mL 4.8604 mL
10 mM 0.2430 mL 1.2151 mL 2.4302 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.08 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.08 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.08 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Sacubitril
Cat. No.:
HY-15407
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