AHU-377 hemicalcium salt MedChemExpress (MCE)

Product Name	AHU-377 hemicalcium salt
Synonyms	(alphar AHU-377 hemicalcium salt AHU-377 (heMicalciuM salt) LCZ696(valsartan + sacubitril) impurity 1 Ethyl (αR,γS)-γ-[(3-carboxy-1-oxopropyl)amino]-α-methyl-[1,1'-biphenyl]-4-pentanoate hemicalcium salt Synonyms (alphar AHU-377 hemicalcium salt AHU-377 (heMicalciuM salt) LCZ696(valsartan + sacubitril) impurity 1 Ethyl (αR,γS)-γ-[(3-carboxy-1-oxopropyl)amino]-α-methyl-[1,1'-biphenyl]-4-pentanoate hemicalcium salt Calciumbis(4-{[(1S,3R)-1-([1,1'-biphenyl]-4-ylmethyl)-4-ethoxy-3-methyl-4-oxobutyl] amino} -4-oxobutanoate)
CAS	1369773-39-6
EINECS
Chemical Formula	C48H56CaN2O10
Molecular Weight	861.04364
inchi
Package	10 mM * 1 mL;2 mg;5 mg;10 mg;25 mg;50 mg;100 mg;200 mg
Price	Email to quote
Descriptions	Sacubitril hemicalcium salt Sacubitril hemicalcium salt MedChemExpress (MCE) HY-15407A 1369773-39-6 AHU-377 hemicalcium salt 99.69% 4°C, sealed storage, away from moisture In solvent : -80°C, 6 months Descriptions Sacubitril hemicalcium salt Sacubitril hemicalcium salt MedChemExpress (MCE) HY-15407A 1369773-39-6 AHU-377 hemicalcium salt 99.69% 4°C, sealed storage, away from moisture In solvent : -80°C, 6 months -20°C, 1 month (sealed storage, away from moisture) Room temperature in continental US may vary elsewhere. 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. 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 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]. 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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Sacubitril hemicalcium salt Related Antibodies \| \| \| \| \| \| \| \| \| \| [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]
Last Update	2025-04-01 14:45:47

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