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1369773-39-6

1369773-39-6 structure
1369773-39-6 structure
  • Name: AHU-377 hemicalcium salt
  • Chemical Name: AHU-377 (heMicalciuM salt)
  • CAS Number: 1369773-39-6
  • Molecular Formula: C24H28Ca0.5NO5
  • Molecular Weight: 430.52
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Neprilysin
  • Create Date: 2018-09-16 20:26:30
  • Modify Date: 2024-01-04 12:53:25
  • Sacubitril (AHU-377) hemicalcium salt is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril hemicalcium salt is a component of the heart failure medicine LCZ696.
Name AHU-377 (heMicalciuM salt)
Synonyms Calcium bis(4-{[(2S,4R)-1-(4-biphenylyl)-5-ethoxy-4-methyl-5-oxo-2-pentanyl]amino}-4-oxobutanoate)
[1,​1'-​Biphenyl]​-​4-​pentanoic acid, γ-​[(3-​carboxy-​1-​oxopropyl)​amino]​-​α-​methyl-​, 4-​ethyl ester, calcium salt (2:1)​, (αR,​γS)​-
[1,1'-Biphenyl]-4-pentanoic acid, γ-[(3-carboxy-1-oxopropyl)amino]-α-methyl-, α-ethyl ester, calcium salt, (αR,γS)- (2:1)
(αR,γS)-γ-[(3-Carboxy-1-oxopropyl)amino]-α-methyl-[1,1'-biphenyl]-4-pentanoic acid 4-ethyl ester calcium salt
(alphaR,gammaS)-gamma-[(3-Carboxy-1-oxopropyl)amino]-alpha-methyl-[1,1'-biphenyl]-4-pentanoic acid 4-ethyl ester calcium salt (2:1)
AHU-377 hemicalcium salt
Description Sacubitril (AHU-377) hemicalcium salt is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril hemicalcium salt is a component of the heart failure medicine LCZ696.
Related Catalog
Target

IC50: 5 nM (NEP)[1]
In Vitro Sacubitril (AHU-377) is a single molecule that is comprised of molecular moieties of valsartan, an ARB, and Sacubitril hemicalcium salt, a neprilysin inhibitor (1:1 ratio). Sacubitril (AHU-377) is converted by enzymatic cleavage of the ethyl ester into the active neprilysin inhibiting metabolite LBQ657[2]. The inactive NEPi precursor, Sacubitril hemicalcium salt, 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 (AHU-377)(tmax 0.5-1.1 h) are absorbed quickly. Sacubitril hemicalcium salt 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 Sacubitril (AHU-377). Urinary volume is also potentiated in animals which receive an iv administration of Sacubitril (AHU-377)[1].
References

[1]. Ksander GM, et al. Dicarboxylic acid dipeptide neutral endopeptidase inhibitors. J Med Chem. 1995 May 12;38(10):1689-700.

[2]. Voors AA, et al. 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, et al. 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.
Molecular Formula C24H28Ca0.5NO5
Molecular Weight 430.52
PSA 191.06000
LogP 5.78240
Storage condition -20℃
Symbol GHS06 GHS09
GHS06, GHS09
Signal Word Danger
Hazard Statements H301-H400
Precautionary Statements Missing Phrase - N15.00950417
Hazard Codes Xi
RIDADR UN2811 - class 6.1 - PG 3 - EHS - Toxic solids, organic, n.o.s., HI: all

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title: CAS No. 1369773-39-6 | Chemsrc address: https://www.chemsrc.com/en/baike/654676.html

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