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

Sacubitril hemicalcium salt (Synonyms: AHU-377 (hemicalcium salt))

Cat. No.: HY-15407A Purity: 99.69% ee.: 99.99%
Handling Instructions

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

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

Sacubitril hemicalcium salt Chemical Structure

Sacubitril hemicalcium salt Chemical Structure

CAS No. : 1369773-39-6

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10 mM * 1 mL in DMSO USD 66 In-stock
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50 mg USD 132 In-stock
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1 g USD 552 In-stock
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Description

Sacubitril hemicalcium salt (AHU-377 hemicalcium salt) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril hemicalcium salt 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 hemicalcium salt, 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 hemicalcium salt, 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 hemicalcium salt 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

430.52

Formula

C₂₄H₂₈Ca₀.₅NO₅

CAS No.

1369773-39-6

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.[0.5Ca2+]

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 : 125 mg/mL (290.35 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3228 mL 11.6139 mL 23.2277 mL
5 mM 0.4646 mL 2.3228 mL 4.6455 mL
10 mM 0.2323 mL 1.1614 mL 2.3228 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: ≥ 6.25 mg/mL (14.52 mM); Clear solution

  • 2.

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

    Solubility: ≥ 6.25 mg/mL (14.52 mM); Clear solution

  • 3.

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

    Solubility: ≥ 6.25 mg/mL (14.52 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.69% ee.: 99.99%

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Sacubitril hemicalcium salt
Cat. No.:
HY-15407A
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