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Sacubitril

Purity: 98.71%
Catalog No. T4574Alias AHU-377, AHU377, AHU 377Cas No. 149709-62-6
Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM and is a component of the heart failure medicine LCZ696.
Pack SizePriceAvailabilityQuantity
5 mg$57In Stock
10 mg$77In Stock
25 mg$116In Stock
50 mg$147In Stock
100 mg$247In Stock
200 mg$368In Stock
500 mg$596In Stock
1 mL x 10 mM (in DMSO)$63In Stock
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Purity:98.71%
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Product Introduction

Bioactivity
Description
Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM and is a component of the heart failure medicine LCZ696.
Targets&IC50
NEP:5 nM 
In vitro
LCZ696 is a single molecule that is comprised of molecular moieties of valsartan, an ARB, and Sacubitril, a neprilysin inhibitor (1:1 ratio). Sacubitril is converted by enzymatic cleavage of the ethyl ester into the active neprilysin inhibiting metabolite LBQ657[2]. The inactive NEPi precursor, Sacubitril, 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 vivo
In humans, Sacubitril (tmax0.5-1.1 h) are absorbed quickly. Sacubitril is converted rapidly into LBQ657 with its tmaxbeing reached in 1.9-3.5 h. Mean t1/2values 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. Urinary volume is also potentiated in animals which receive an iv administration of Sacubitril[1].
AliasAHU-377, AHU377, AHU 377
Chemical Properties
Molecular Weight411.49
FormulaC24H29NO5
Cas No.149709-62-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 27.5 mg/mL (66.83 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4302 mL12.1510 mL24.3019 mL121.5096 mL
5 mM0.4860 mL2.4302 mL4.8604 mL24.3019 mL
10 mM0.2430 mL1.2151 mL2.4302 mL12.1510 mL
20 mM0.1215 mL0.6075 mL1.2151 mL6.0755 mL
50 mM0.0486 mL0.2430 mL0.4860 mL2.4302 mL

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