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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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İçerik

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


Adı4-(((2S,4R)-1-([1,1'-biphenyl]-4-yl)-5-ethoxy-4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoic acid
EşanlamlarAHU-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'ın149709-62-6
EINECS'in1592732-453-0
Moleküler FormülC24H29NO5
Molar Kütlesi411.49
Yoğunluk1.151±0.06 g/cm3(Önceden)
Boling Point656.9±55.0 °C(Predicted)
ÇözünürlükDMSO'da 10 mM
pKa4.72±0.10(Predicted)
Depolama Koşulları- 20°C altındaki buzdolabı, kuruyu, dondurma deposu.
KullanımAraştırma
In vitro çalışmaSacubitril (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 çalışmaIn 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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