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

Sacubitrilat  (Synonyms: Desethyl Sacubitril; LBQ-657)

Cat. No.: HY-17620 Purity: 99.00%
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Sacubitrilat (Desethyl Sacubitril) 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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 132 In-stock
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Solid
1 mg USD 40 In-stock
5 mg USD 120 In-stock
10 mg USD 200 In-stock
25 mg USD 440 In-stock
50 mg USD 700 In-stock
100 mg USD 1120 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Sacubitrilat:

Sacubitrilat Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Sacubitrilat (Desethyl Sacubitril) 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Sacubitrilat Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

383.44

Formula

C22H25NO5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

[H]N(C(CCC(O)=O)=O)[C@H](CC(C=C1)=CC=C1C2=CC=CC=C2)C[C@H](C(O)=O)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (260.80 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6080 mL 13.0398 mL 26.0797 mL 65.1992 mL
5 mM 0.5216 mL 2.6080 mL 5.2159 mL 13.0398 mL
10 mM 0.2608 mL 1.3040 mL 2.6080 mL 6.5199 mL
15 mM 0.1739 mL 0.8693 mL 1.7386 mL 4.3466 mL
20 mM 0.1304 mL 0.6520 mL 1.3040 mL 3.2600 mL
25 mM 0.1043 mL 0.5216 mL 1.0432 mL 2.6080 mL
30 mM 0.0869 mL 0.4347 mL 0.8693 mL 2.1733 mL
40 mM 0.0652 mL 0.3260 mL 0.6520 mL 1.6300 mL
50 mM 0.0522 mL 0.2608 mL 0.5216 mL 1.3040 mL
60 mM 0.0435 mL 0.2173 mL 0.4347 mL 1.0867 mL
80 mM 0.0326 mL 0.1630 mL 0.3260 mL 0.8150 mL
100 mM 0.0261 mL 0.1304 mL 0.2608 mL 0.6520 mL
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Sacubitrilat Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Sacubitrilat149709-44-4Desethyl Sacubitril LBQ-657LBQ657LBQ 657LBQ-657NeprilysinNeutral endopeptidaseNEPCluster of differentiation 10CD10Inhibitorinhibitorinhibit

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