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Sacubitril hemicalcium salt

🥰Excellent
Catalog No. T4200Cas No. 1369773-39-6
Alias AHU377 calcium salt, AHU-377 (hemicalcium salt)

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.

Sacubitril hemicalcium salt
Other Forms of Sacubitril hemicalcium salt:

Sacubitril hemicalcium salt

🥰Excellent
Purity: 99.93%
Catalog No. T4200Alias AHU377 calcium salt, AHU-377 (hemicalcium salt)Cas 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.
Pack SizePriceAvailabilityQuantity
2 mg$33In Stock
5 mg$48In Stock
10 mg$58In Stock
25 mg$86In Stock
50 mg$108In Stock
100 mg$157In Stock
200 mg$217In Stock
1 mL x 10 mM (in DMSO)$58In Stock
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Purity:99.93%
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COA HNMR HPLC
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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.
Targets&IC50
NEP:5 nM
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.
AliasAHU377 calcium salt, AHU-377 (hemicalcium salt)
Chemical Properties
Molecular Weight861.06
FormulaC48H56CaN2O10
Cas No.1369773-39-6
Smiles[Ca++].CCOC(=O)[C@H](C)C[C@@H](Cc1ccc(cc1)-c1ccccc1)NC(=O)CCC([O-])=O.CCOC(=O)[C@H](C)C[C@@H](Cc1ccc(cc1)-c1ccccc1)NC(=O)CCC([O-])=O
Relative Density.1.24 g/cm3 at 20℃
Storage & Solubility Information
Storagekeep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 60 mg/mL (69.68 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.1614 mL5.8068 mL11.6136 mL58.0680 mL
5 mM0.2323 mL1.1614 mL2.3227 mL11.6136 mL
10 mM0.1161 mL0.5807 mL1.1614 mL5.8068 mL
20 mM0.0581 mL0.2903 mL0.5807 mL2.9034 mL
50 mM0.0232 mL0.1161 mL0.2323 mL1.1614 mL

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Keywords

Cluster of differentiation 10NeprilysinAHU-377AHU377Sacubitril hemicalcium saltNEPinhibitCD10Sacubitril hemicalciumSacubitrilNeutral endopeptidaseAHU 377AHU-377 hemicalciumAHU377 calciumInhibitor
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