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[CAS NO. 1369773-39-6] Sacubitrilhemicalciumsalt
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-15407A |
| Brand: | MCE |
| CAS: | 1369773-39-6 |
Overview
| MDL | MFCD28137893 |
|---|---|
| Molecular Weight | 430.52 |
| Molecular Formula | C24H28Ca0.5NO5 |
| 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+] |
1 Publications Citing Use of MCE
Summary
Sacubitril hemicalcium salt (AHU-377 hemicalcium salt) is a potent NEP inhibitor with an IC 50 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
In humans, Sacubitril (AHU-377)(t max 0.5-1.1 h) are absorbed quickly. Sacubitril hemicalcium salt is converted rapidly into LBQ657 with its t max being reached in 1.9-3.5 h. Mean t 1/2 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT05117736 | Montreal Heart Institute|Novartis Pharmaceuticals |
Systemic Right Ventricle|Heart Failure
|
March 15, 2022 | Not Applicable |
| NCT05580510 | Instituto Nacional de Cardiologia Ignacio Chavez|Boehringer Ingelheim laboratory |
Congenital Heart Disease|Heart Failure|Heart Failure With Reduced Ejection Fraction
|
February 6, 2023 | Phase 2|Phase 3 |
| NCT04883528 | Duke University|Novartis Pharmaceuticals |
Covid19
|
August 6, 2021 | Phase 1|Phase 2 |
| NCT05498675 | Beijing Friendship Hospital |
Sacubitril+Valsartan|Hypertension|Obesity
|
September 1, 2021 | |
| NCT04218435 | Clinision |
Heart Failure NYHA Class IV|Heart Failure NYHA Class II
|
January 1, 2019 | |
| NCT04572724 | Shenzhen Second People´s Hospital |
Peritoneal Dialysis Complication|Hemodialysis Complication|Heart Failure
|
July 6, 2020 | Phase 4 |
| NCT03553303 | Oslo University Hospital |
Heart Failure, Systolic
|
October 16, 2018 | Phase 4 |
| NCT05164653 | WDB Clinical Research Co., Ltd. |
Heart Failure
|
December 27, 2021 | Phase 4 |
| NCT04149990 | Jacob Moller|Danish Heart Foundation|Odense University Hospital|Rigshospitalet, Denmark |
Myocardial Infarction|Diastolic Dysfunction
|
October 12, 2018 | Phase 2 |
| NCT04753112 | Germans Trias i Pujol Hospital |
Pulmonary Hypertension
|
October 29, 2020 | Phase 3 |
| NCT01281306 | Novartis Pharmaceuticals|Novartis |
Systolic Hypertension
|
January 2011 | Phase 2 |
| NCT04458285 | Guangdong Provincial People´s Hospital |
Hemodialysis Complication|Heart Failure
|
January 1, 2020 | Not Applicable |
| NCT02916160 | University Hospital, Montpellier |
Chronic Heart Failure|Sleep Apnea Syndrome
|
September 22, 2016 | Phase 4 |
| NCT04853758 | University of Sao Paulo General Hospital|InCor Heart Institute |
Chagas Cardiomyopathy
|
May 6, 2021 | Phase 3 |
| NCT03893435 | The Young Investigator Group of Cardiovascular Research |
Acute Myocardial Infarction
|
December 1, 2018 | Not Applicable |
| NCT00549770 | Novartis Pharmaceuticals|Novartis |
Hypertension
|
September 2007 | Phase 2 |
| NCT04197050 | RenJi Hospital |
Myocardial Injury|Connective Tissue Diseases
|
February 20, 2020 | Phase 4 |
| NCT05508035 | John Paul II Hospital, Krakow |
Heart Failure With Moderately Reduced Ejection Fraction
|
September 15, 2022 | Phase 3 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 125 mg/mL ( 290.35 mM ; Need ultrasonic)
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 |
References
- [1] Ksander GM, et al. Dicarboxylic acid dipeptide neutral endopeptidase inhibitors. J Med Chem. 1995 May 12;38(10):1689-700.
- [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.
- [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.
Synonyms
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