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Sacubitril hemicalcium salt

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Purity:99.28%

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COA HPLC LCMS HNMR

Sacubitril hemicalcium salt

Catalog No. T4200Cas No. 1369773-39-6

Sacubitril hemicalcium salt (AHU377 calcium salt) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril hemicalcium salt is a component of the heart failure medicine LCZ696. Sacubitril hemicalcium salt is a prodrug of LBQ657, which is an inhibitor of the zinc metallopeptidase neprilysin. Neprilysin degrades a variety of vasoactive peptides such as atrial and brain natriuretic peptide, bradykinin, adrenomedullin, and endothelin-1. Inhibition of neprilysin leads to an increased level of these peptides and, thus, antihypertensive effects. Formulations containing AHU377 in combination with the angiotensin II receptor antagonist valsartan are used to treat hypertension and heart failure.

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Pack Size	Price	Availability
2 mg	$33	In Stock
5 mg	$48	In Stock
10 mg	$58	In Stock
25 mg	$86	In Stock
50 mg	$108	In Stock
100 mg	$157	In Stock
200 mg	$217	In Stock
1 mL x 10 mM (in DMSO)	$58	In Stock

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Product Introduction

Bioactivity

Description	Sacubitril hemicalcium salt (AHU377 calcium salt) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril hemicalcium salt is a component of the heart failure medicine LCZ696. Sacubitril hemicalcium salt is a prodrug of LBQ657, which is an inhibitor of the zinc metallopeptidase neprilysin. Neprilysin degrades a variety of vasoactive peptides such as atrial and brain natriuretic peptide, bradykinin, adrenomedullin, and endothelin-1. Inhibition of neprilysin leads to an increased level of these peptides and, thus, antihypertensive effects. Formulations containing AHU377 in combination with the angiotensin II receptor antagonist valsartan are used to treat hypertension and heart failure.
In vitro	AHU377 is converted by enzymatic cleavage of the ethyl ester into the active neprilysin inhibiting metabolite LBQ657. 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.
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.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.
Alias	AHU-377 (hemicalcium salt), AHU377 calcium salt

Chemical Properties

Molecular Weight	861.06
Formula	C48H56CaN2O10
Cas No.	1369773-39-6

Storage & Solubility Information

Storage

keep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 60 mg/mL (69.68 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.1614 mL	5.8068 mL	11.6136 mL	58.0680 mL
5 mM	0.2323 mL	1.1614 mL	2.3227 mL	11.6136 mL
10 mM	0.1161 mL	0.5807 mL	1.1614 mL	5.8068 mL
20 mM	0.0581 mL	0.2903 mL	0.5807 mL	2.9034 mL
50 mM	0.0232 mL	0.1161 mL	0.2323 mL	1.1614 mL

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