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

Sacubitrilat (Synonyms: LBQ-657)

Cat. No.: HY-17620 Purity: 99.85%
Handling Instructions

Sacubitrilat is an active neprilysin (NEP) inhibitor.

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

Sacubitrilat Chemical Structure

Sacubitrilat Chemical Structure

CAS No. : 149709-44-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 233 In-stock
Estimated Time of Arrival: December 31
2 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 276 In-stock
Estimated Time of Arrival: December 31
10 mg USD 468 In-stock
Estimated Time of Arrival: December 31
25 mg USD 948 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1320 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Description

Sacubitrilat is an active neprilysin (NEP) inhibitor.

IC50 & Target

Neprilysin[1]

In Vitro

Sacubitrilat (LBQ657) is a single diastereomer with specific stereocenters. 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 (LBQ657), and valsartan following the administration of single oral doses of LCZ696 400 or 1200 mg under fasting condition 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. The arithmetic mean AUC0-24 h and AUClast for Sacubitril and Sacubitrilat increases approximately dose proportionally, but shows less than dose proportional increase for Valsartan[2].

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 (260.80 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6080 mL 13.0399 mL 26.0797 mL
5 mM 0.5216 mL 2.6080 mL 5.2159 mL
10 mM 0.2608 mL 1.3040 mL 2.6080 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

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

383.44

Formula

C₂₂H₂₅NO₅

CAS No.

149709-44-4

SMILES

[H]N(C(CCC(O)=O)=O)[[email protected]](CC(C=C1)=CC=C1C2=CC=CC=C2)C[[email protected]](C(O)=O)C

Shipping

Room temperature in continental US; may vary elsewhere

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The dilution calculator equation

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

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Product Name:
Sacubitrilat
Cat. No.:
HY-17620
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Sacubitrilat

Cat. No.: HY-17620