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AHU-377(Sacubitril)

Catalog No.
B1070
Neprilysin inhibitor
Grouped product items
SizePriceStock Qty
5mg
$70.00
In stock
10mg
$95.00
In stock
50mg
$180.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

AHU-377 is an inhibitor of neprilysin with IC50 value of 5nM [1].

AHU-377 and the angiotensin II AT1 receptor antagonist valsartan compose LCZ696 in a 1:1 molar ratio. LCZ696 is an angiotensin receptor neprilysin inhibitor. It can reduce blood pressure and may be a novel drug for the treatment of heart failure. AHU-377 is a prodrug, it can be converted by enzymatic cleavage of the ethyl ester into the active form LBQ657. It is reported that AHU-377(30 and 100 mg/kg, PO) can cause antihypertensive effect in a dose-dependent manner in Dahl-SS rats. But in the DOCA-salt hypertensive rats, it shows a weak reduction [2, 3].

References:
[1] Ksander GM, Ghai RD, deJesus R, Diefenbacher CG, Yuan A, Berry C, Sakane Y, Trapani A. Dicarboxylic acid dipeptide neutral endopeptidase inhibitors. J Med Chem. 1995 May 12;38(10):1689-700.
[2] Voors AA, Dorhout B, van der Meer P. The potential role of valsartan + AHU377 ( LCZ696 ) in the treatment of heart failure. Expert Opin Investig Drugs. 2013 Aug;22(8):1041-7.
[3] Laxminarayan G Hegde, Cecile Yu, Cheruvu Madhavi et al. Comparative efficacy of AHU-377, a potent neprilysin inhibitor, in two rat models of volume-dependent hypertension. BMC Pharmacology 2011, 11(Suppl 1):P33.

Chemical Properties

Physical AppearanceA colorless oil
StorageStore at -20°C
M.Wt411.49
Cas No.149709-62-6
FormulaC24H29NO5
SynonymsSacubitril
Solubility≥41.1 mg/mL in DMSO; ≥21.45 mg/mL in H2O with ultrasonic; ≥26.85 mg/mL in EtOH with ultrasonic
Chemical Name4-[[(2S,4R)-5-ethoxy-4-methyl-5-oxo-1-(4-phenylphenyl)pentan-2-yl]amino]-4-oxobutanoic acid
SDFDownload SDF
Canonical SMILESCCOC(=O)C(C)CC(CC1=CC=C(C=C1)C2=CC=CC=C2)NC(=O)CCC(=O)O
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Biological Activity

Description AHU-377 is an inhibitor of neprilysin with IC50 value of 5 nM.
Targets neprilysin          
IC50 5 nM          

Quality Control