AHU-377 (heMicalciuM salt)
AHU-377 (heMicalciuM salt) Basic information
- Product Name:
- AHU-377 (heMicalciuM salt)
- Synonyms:
-
- AHU-377 (heMicalciuM salt)
- (alphaR,gammaS)-gamma-[(3-Carboxy-1-oxopropyl)amino]-alpha-methyl-[1,1'-biphenyl]-4-pentanoic acid 4-ethyl ester calcium salt (2:1)
- (2S,4R)-5-(Biphenyl-4-yl)-4-[(3-carboxypropionyl)amino]-2-methylpentanoic acid ethyl ester,calcium salt(2:1)
- AHU-377 hemicalcium salt (2:1)
- Calciumbis(4-{[(1S,3R)-1-([1,1'-biphenyl]-4-ylmethyl)-4-ethoxy-3-methyl-4-oxobutyl] amino} -4-oxobutanoate)
- LCZ696(valsartan + sacubitril) impurity 1
- Ethyl (αR,γS)-γ-[(3-carboxy-1-oxopropyl)amino]-α-methyl-[1,1'-biphenyl]-4-pentanoate hemicalcium salt
- (alphar
- CAS:
- 1369773-39-6
- MF:
- C48H56CaN2O10
- MW:
- 861.04364
- EINECS:
- 935-847-3
- Product Categories:
-
- Intermediates
- LCZ 696
- Pharmaceutical Intermediates
- lcz696
- 1369773-39-6
- Mol File:
- 1369773-39-6.mol
AHU-377 (heMicalciuM salt) Chemical Properties
- Melting point:
- >140°C (dec.)
- Density
- 1.24g/cm3 at 20℃
- vapor pressure
- 0.001Pa at 20℃
- storage temp.
- -20°C
- solubility
- DMSO (Slightly, Heated), Methanol (Slightly)
- form
- powder
- color
- white to beige
- optical activity
- -16.3°(C=0.01g/mL,MEOH, 20°C, 589nm)
- InChIKey
- DDLCKLBRBPYKQS-AGIGYYLVNA-L
- LogP
- -0.66-2.9 at 20℃ and pH2-7
AHU-377 (heMicalciuM salt) Usage And Synthesis
Uses
Sacubitril is an antihypertensive drug used in combination with valsartan. The combination drug, valsartan/sacubitril, known during trials as LCZ696 and marketed under the brand name, Entresto, is a treatment for heart failure.
Biochem/physiol Actions
Sacubitril (AHU377) is a prodrug inhibitor of the membrane metallo-endopeptidase neprilysin. Sacubitril forms half of the heart failure combination drug LCZ696, along with the angiotensin-receptor blocker Valsartan. Sacubitril (AHU377) is cojnverted by esterases into the active inhibitor LBQ657, which prevents neprilysin′s degradation of atrial and brain natriuretic peptide, two blood pressure lowering peptides. The AHU377 valsartan combination drug LCZ696 showed a reduction in the risk of cardiovascular death of 20% compared to the standard ACE inhibitor enalapril, and also a 21% drop in the risk of hospitalization.
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].
storage
Store at -20°C
AHU-377 (heMicalciuM salt)Supplier
- Tel
- 0519-83984084
- sales@ydpharm.com
- Tel
- 025-58741518 13327700685
- sales@vcarepharmatech.com
- Tel
- sales@boylechem.com
- Tel
- 18515581800 18501085097
- sales.bj@hwrkchemical.com
- Tel
- 21-21-54301573 13917723525
- sales@scientiapharm.com
AHU-377 (heMicalciuM salt)(1369773-39-6)Related Product Information
- Sacubitril-(2R,4R)-Isomer
- Sacubitril - D4
- AHU-377
- (2R,4S)-5-([1,1'-biphenyl]-4-yl)-4-aMino-2-Methylpentanoic acid hydrochloride
- LCZ696
- (R,E)-5-([1,1'-biphenyl]-4-yl)-4-((tert-butoxycarbonyl)aMino)-2-Methylpent-2-enoic acid
- LCZ696 interMediate
- (2S,4S)-5-(Biphenyl-4-yl)-4-[(tert-butoxycarbonyl)amino]-2-methylpentanoic acid
- (2R,4S)-4-([1,1'-Biphenyl]-4-ylmethyl)-2-methyl-4-(2,5-dioxopyrrolidin-1-yl)butanoic acid
- (S)-5-[(Biphenyl-4-yl)methyl]-1-(2,2-dimethylpropionyl)pyrrolidin-2-one
- Sacubitril Impurity 72
- (2R,4S)-4-([1,1'-Biphenyl]-4-ylmethyl)-4-(4-ethoxy-4-oxobutanamido)-2-methylbutanoic acid
- ((R)-2-biphenyl-4-yl-1-forMylethyl)carbaMic acid t-butyl ester
- 2-Pyrrolidinone, 5-([1,1'-biphenyl]-4-ylMethyl)-3-Methyl-, (3R,5S)-
- Ethyl (2R,4S)-4-([1,1'-biphenyl]-4-ylmethyl)-2-methyl-4-(2,5-dioxopyrrolidin-1-yl)butanoate
- sacubitril
- Valsartan
- (2R,4S)-5-([1,1'-biphenyl]-4-yl)-4-((tert-butoxycarbonyl)aMino)-2-Methylpentanoic acid
- Sacubitril Calcium