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

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, o...

Introduction

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

Name 4-(((2S,4R)-1-([1,1′-biphenyl]-4-yl)-5-ethoxy-4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoic acid
Synonyms AHU-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
CAS 149709-62-6
EINECS 1592732-453-0
Molecular Formula C24H29NO5
Molar Mass 411.49
Density 1.151±0.06 g/cm3(Predicted)
Boling Point 656.9±55.0 °C(Predicted)
Solubility 10 mM in DMSO
pKa 4.72±0.10(Predicted)
Storage Condition Sealed in dry,Store in freezer, under -20°C
Use Intermediate
In vitro study Sacubitril (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.
In vivo study In 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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