Chemical Name:AHU-377CAS No.: 149709-62-6Assay: ≥99%Appearance:colorless transparent oily liquid
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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
| Nome | 4-(((2S,4R)-1-([1,1'-biphenyl]-4-yl)-5-ethoxy-4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoic acid |
| Sinonimi | 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 |
| Formula molecolare | C24H29NO5 |
| massa molare | 411.49 |
| Densità | 1.151±0.06 g/cm3(Predicted) |
| punto Boling | 656.9±55.0 °C(Predicted) |
| Solubilità | 10 mM in DMSO |
| pKa | 4.72±0.10(Predicted) |
| Condizioni di conservazione | Sealed in dry,Store in freezer, under -20°C |
| Utilizzo | 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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