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AHU-377 CAS No.:149709-62-6

Chemical Name:AHU-377CAS No.: 149709-62-6Assay: ≥99%Appearance:colorless transparent oily liquid

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Contenido

AHU-377 Usage: Used as pharmaceutical intermediate AHU-377 Packaging and Shipping: 25kg/ drum or as per buyer requirement. AHU-377 Storage: Ventilated and dry; separate from alkalis, oxidisers, organic materials and flammable materials


Nombre4-(((2S,4R)-1-([1,1'-biphenyl]-4-yl)-5-ethoxy-4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoic acid
SinónimosAHU-37
AHU377
AHU-377
AHU 377
SACUBITRIL
AHU-377,149709-62-6
(2R,4S)-5-([1,1'-Biphenyl]-4-yl)-4-(3-carboxypropanamido)-2-methylpentanoic acid
(2R,4S)-5-(Biphenyl-4-yl)-4-[(3-carboxypropionyl)amino]-2-methylpentanoic acid ethyl ester
4-(((2S,4R)-1-([1,1'-biphenyl]-4-yl)-5-ethoxy-4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoic acid
4-(((2R,4R)-1-([1,1'-biphenyl]-4-yl)-5-ethoxy-4-Methyl-5-oxopentan-2-yl)aMino)-4-oxobutanoic acid
4-(((2S,4R)-1-([1,1'-biphenyl]-4-yl)-5-ethoxy-4-Methyl-5-oxopentan-2-yl)aMino)-4-oxobutanoic acid
CAS149709-62-6
EINECS1592732-453-0
Fórmula MolecularC24H29NO5
Masa Molar411.49
Densidad1.151±0.06 g/cm3(Predicted)
punto Boling656.9±55.0 °C(Predicted)
Solubilidad10 mM in DMSO
PKa4.72±0.10(Predicted)
Condición de almacenamientoSealed in dry,Store in freezer, under -20°C
UsoIntermediate
Estudio in vitroSacubitril (AHU-377) is a single molecule that is comprised of molecular moieties of valsartan, an ARB, and Sacubitril (AHU-377), 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. The inactive NEPi precursor, Sacubitril (AHU-377), 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.
Estudio in vivoIn humans, Sacubitril (AHU-377) (t max 0.5-1.1 h) are absorbed quickly. Sacubitril (AHU-377) 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. 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).

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