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Sacubitril

Catalog No. T4574 CAS 149709-62-6

Synonyms: AHU 377, AHU377, AHU-377

Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril is a component of the heart failure medicine LCZ696.

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Sacubitril, CAS 149709-62-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 57.00
10 mg	In stock	$ 77.00
25 mg	In stock	$ 116.00
50 mg	In stock	$ 147.00
100 mg	In stock	$ 247.00
200 mg	In stock	$ 368.00
500 mg	In stock	$ 596.00
1 mL * 10 mM (in DMSO)	In stock	$ 63.00

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Purity: 98.71%

Purity: 98.28%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril 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 AHU377, a neprilysin inhibitor (1:1 ratio). AHU377 is converted by enzymatic cleavage of the ethyl ester into the active neprilysin inhibiting metabolite LBQ657[2]. The inactive NEPi precursor, AHU377, 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, AHU377 (tmax?0.5-1.1 h) are absorbed quickly. AHU377 is converted rapidly into LBQ657 with its tmax?being reached in 1.9-3.5 h. Mean t1/2?values 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 AHU377. Urinary volume is also potentiated in animals which receive an iv administration of AHU377[1].

Synonyms	AHU 377, AHU377, AHU-377
Molecular Weight	411.49
Formula	C24H29NO5
CAS No.	149709-62-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 27.5 mg/mL (66.83 mM)

References and Literature

1. Ksander GM,etal.Dicarboxylic acid dipeptide neutral endopeptidase inhibitors.J Med Chem. 1995 May 12;38(10):1689-700. 2. Voors AA,etal.The potential role of valsartan + AHU377 ( LCZ696 ) in the treatment of heart failure.Expert Opin Investig Drugs. 2013 Aug;22(8):1041-7. 3. von Lueder TG,etal.Angiotensin receptor neprilysin inhibitor LCZ696 attenuates cardiac remodeling and dysfunction after myocardial infarction by reducing cardiac fibrosis and hypertrophy. Circ Heart Fail. 2015 Jan;8(1):71-8.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library EMA Approved Drug Library Drug Repurposing Compound Library Anti-Hypertension Compound Library FDA-Approved & Pharmacopeia Drug Library Anti-COVID-19 Compound Library FDA-Approved Drug Library Metabolism Compound Library Anti-Metabolism Disease Compound Library Pediatric Drug Library

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Keywords

Sacubitril 149709-62-6 Metabolism Neprilysin Neutral endopeptidase AHU 377 inhibit NEP antihypertensive AHU377 natriuretic peptide AHU-377 Cluster of differentiation 10 Inhibitor COVID-19 CD10 heart failure inhibitor

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