Sacubitril hemicalcium salt
Based on 3 publication(s) in Google Scholar
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.
- Purity: 99.82%
- CAS No.: 1369773-39-6
- Formula: C24H28Ca0.5NO5
- Molecular Weight:430.52
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Sacubitril hemicalcium salt
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ELISA
Biological Activity
IC50: 5 nM (NEP)[1]
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1369773-39-6
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Appearance Solid
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Molecular Weight 430.52
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Formula C24H28Ca0.5NO5
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Color White to off-white
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SMILES
O=C(CCC([O-])=O)N[C@H](CC1=CC=C(C2=CC=CC=C2)C=C1)C[C@@H](C)C(OCC)=O.[0.5Ca2+]
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Synonyms
AHU-377 hemicalcium salt
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Theranostics
Activating AhR alleviates cognitive deficits of Alzheimer's disease model mice by upregulating endogenous Aβ catabolic enzyme Neprilysin. [Abstract]2021 Aug 11;11(18):8797-8812. PMID: 34522212
Sacubitril hemicalcium salt purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Aug 11;11(18):8797-8812. [Abstract]
N2a-APP cells were treated with Diosmin (Dio; 80 μM), FICZ (250 nM), L-KN (3 μM) or Indole-3-acetamide (I3C; 10 μM) with or without SR1 (2 μM) or Sacubitril (Sac; 1 μM) for 24 h, the supernatant was collected and the Aβ42 levels were determined by ELISA.
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Cardiovasc Diabetol
Sacubitril/Valsartan partially alleviates myocardial infarction injury by activating the FGF21 signaling pathway via PPARs. [Abstract]2025 Feb 22;24(1):89. PMID: 39987117 -
Mol Biol Rep
Cardiac drug potential: exploring individual and combined cardiac drugs to promote differentiation of adipose-derived stem cells into cardiomyocytes. [Abstract]2026 Feb 26;53(1):434. PMID: 41746444
Solvent & Solubility
DMSO : 125 mg/mL (290.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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.
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
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (277 KB)
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SDS (623 KB)
- English - EN (623 KB)
- Français - FR (623 KB)
- Deutsch - DE (623 KB)
- Norwegian - NO (623 KB)
- Español - ES (623 KB)
- Swedish - SV (623 KB)
- Italian - IT (623 KB)
- Korean - KR (623 KB)
- Portuguese - PT (623 KB)
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Handling Instructions (2659 KB)
References
[1]. Ksander GM, et al. Dicarboxylic acid dipeptide neutral endopeptidase inhibitors. J Med Chem. 1995 May 12;38(10):1689-700. [Content Brief]
[2]. Voors AA, et al. The potential role of valsartan + AHU377 ( LCZ696 ) in the treatment of heart failure. Expert Opin Investig Drugs. 2013 Aug;22(8):1041-7. [Content Brief]
[3]. von Lueder TG, et al. Angiotensin receptor neprilysin inhibitor LCZ696 attenuates cardiac remodeling and dysfunction after myocardial infarction by reducing cardiac fibrosis and hypertrophy. Circ Heart Fail. 2015 Jan;8(1):71-8. [Content Brief]
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.3228 mL | 11.6139 mL | 23.2277 mL | 58.0693 mL |
| 5 mM | 0.4646 mL | 2.3228 mL | 4.6455 mL | 11.6139 mL | |
| 10 mM | 0.2323 mL | 1.1614 mL | 2.3228 mL | 5.8069 mL | |
| 15 mM | 0.1549 mL | 0.7743 mL | 1.5485 mL | 3.8713 mL | |
| 20 mM | 0.1161 mL | 0.5807 mL | 1.1614 mL | 2.9035 mL | |
| 25 mM | 0.0929 mL | 0.4646 mL | 0.9291 mL | 2.3228 mL | |
| 30 mM | 0.0774 mL | 0.3871 mL | 0.7743 mL | 1.9356 mL | |
| 40 mM | 0.0581 mL | 0.2903 mL | 0.5807 mL | 1.4517 mL | |
| 50 mM | 0.0465 mL | 0.2323 mL | 0.4646 mL | 1.1614 mL | |
| 60 mM | 0.0387 mL | 0.1936 mL | 0.3871 mL | 0.9678 mL | |
| 80 mM | 0.0290 mL | 0.1452 mL | 0.2903 mL | 0.7259 mL | |
| 100 mM | 0.0232 mL | 0.1161 mL | 0.2323 mL | 0.5807 mL |
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