Pharmacologic action Novartis’ New Angiomyocardiac LCZ696 Market analysis
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AHU-377

Pharmacologic action Novartis’ New Angiomyocardiac LCZ696 Market analysis
Product Name
AHU-377
CAS No.
149709-62-6
Chemical Name
AHU-377
Synonyms
Sacubitril(AHU-377);Sacubitril API;valsartan/sacubitril Impurity 1;(2R,4S)-5-([1,1'-Biphenyl]-4-yl)-4-(3-carboxypropanamido)-2-methylpentanoic acid;AHU-37;AHU-77;LCZ697;AHU-377;SACUBRITIL;LCZ-696-007-2S4R
CBNumber
CB62627304
Molecular Formula
C24H29NO5
Formula Weight
411.49
MOL File
149709-62-6.mol
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AHU-377 Property

Boiling point:
656.9±55.0 °C(Predicted)
Density 
1.151±0.06 g/cm3(Predicted)
storage temp. 
Sealed in dry,Store in freezer, under -20°C
solubility 
≥41.1 mg/mL in DMSO; ≥21.45 mg/mL in H2O with ultrasonic; ≥26.85 mg/mL in EtOH with ultrasonic
form 
oil
pka
4.72±0.10(Predicted)
color 
colorless
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

TRC
Product number
S080895
Product name
Sacubitril
Packaging
250mg
Price
$580
Updated
2021/12/16
TRC
Product number
S080895
Product name
Sacubitril
Packaging
500mg
Price
$1115
Updated
2021/12/16
Matrix Scientific
Product number
132790
Product name
4-(((2S,4R)-1-([1,1'-Biphenyl]-4-yl)-5-ethoxy-4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoicacid
Purity
97%
Packaging
5g
Price
$1980
Updated
2021/12/16
ApexBio Technology
Product number
B1070
Product name
AHU-377(Sacubitril)
Packaging
50mg
Price
$885
Updated
2021/12/16
Matrix Scientific
Product number
132790
Product name
4-(((2S,4R)-1-([1,1'-Biphenyl]-4-yl)-5-ethoxy-4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoicacid
Purity
97%
Packaging
1g
Price
$648
Updated
2021/12/16
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AHU-377 Chemical Properties,Usage,Production

Pharmacologic action

AHU377 and angiotensin IIAT1 receptor antagonist valsartan at a molar ratio of 1: 1 compose LCZ696. LCZ696 was a dual inhibitor of angiotensin II (AT2) receptor and enkephalinase (Neprilysin) receptor. And with its better antihypertensive efficacy than standard antihypertensive drugs, it is a new drug for the treatment of heart failure.
AHU377 is a prodrug that converts the active form of the enzyme cleavage LBQ657 ethyl ester. So far its efficacy and safety in milestone phase III surpass the clinical standard drug enalapril.
In a clinical trial of the drug, 100 to 400 mg of combined drugs, 80 to 320 mg of valsartan, 200 mg of neprilysin inhibition or placebo were given to the patients in the double-blind trial of phase two with mild to moderate hypertension. The combined drugs are more effective and better tolerated with no vascular edema report than solely applied valsartan or other drugs. LCZ696 shows sustainable treatment benefits in the early treatment:
(1) a 20% reduction in the risk of death from cardiovascular disease (p = 0.00004).
(2) hospitalization for heart failure was reduced by 21% (p = 0.00004).
(3) all-cause mortality was reduced by 16% (p = 0.0005).
(4) The overall risk is reduced by 20% according to the composite measure of the primary endpoint of hospitalization for cardiovascular death or heart failure (p = 0.0000002).

Novartis’ New Angiomyocardiac LCZ696

According to a recent study published by Novartis, LCZ696, a cardiovascular drug being developed by the company, will become a new hope for the company. The current study shows that this drug functions well in the remission of cardiovascular necrosis and other symptoms caused by heart disease.
LCZ696 is a combination of Novartis Diovan and AHU-377. Some analysts have spoken highly of the drug and estimated that it might be submitted to the FDA as early as next year. Once confirmed in the audit it will mark another great step forward of Novartis in the field of cardiovascular drugs.
Although it showed high expectations to LCZ696, Novartis still has a long way to go, given the setbacks of its serelaxin in the FDA and the European Medicines Administration.
The news came straight from Basel as investigators around the world were wrapping up the big scientific meeting of the American College of Cardiology.

Market analysis

In the field of research and development of drugs, most of the success of the new drugs in phase II will always lead to a series of competitor projects. The LCZ696 performs so prominently that the industry was shocked. It is predicted that few cardiovascular drugs will be qualified to compete with the LCZ696 in the next few years. Some analysts predict that the LCZ696 sales will peak at $ 8 billion, while Deutsche Bank analysts expect the drug to peak at $ 6 billion, given LCZ696's superior performance in reducing cardiovascular risk. Although the data are slightly different, there is no doubt that, LCZ696 will become a super star to lead the cardiovascular treatment to step into a new era.

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.

Definition

ChEBI: Sacubitril is a member of biphenyls.

Biological Activity

ahu-377 is an inhibitor of neprilysin with ic50 value of 5nm [1].ahu-377 and the angiotensin ii at1 receptor antagonist valsartan compose lcz696 in a 1:1 molar ratio. lcz696 is an angiotensin receptor neprilysin inhibitor. it can reduce blood pressure and may be a novel drug for the treatment of heart failure. ahu-377 is a prodrug, it can be converted by enzymatic cleavage of the ethyl ester into the active form lbq657. it is reported that ahu-377(30 and 100 mg/kg, po) can cause antihypertensive effect in a dose-dependent manner in dahl-ss rats. but in the doca-salt hypertensive rats, it shows a weak reduction [2, 3].

target

neprilysin

References

[1] ksander gm, ghai rd, dejesus r, diefenbacher cg, yuan a, berry c, sakane y, trapani a. dicarboxylic acid dipeptide neutral endopeptidase inhibitors. j med chem. 1995 may 12;38(10):1689-700.
[2] voors aa, dorhout b, van der meer p. the potential role of valsartan + ahu377 ( lcz696 ) in the treatment of heart failure. expert opin investig drugs. 2013 aug;22(8):1041-7.
[3] laxminarayan g hegde, cecile yu, cheruvu madhavi et al. comparative efficacy of ahu-377, a potent neprilysin inhibitor, in two rat models of volume-dependent hypertension. bmc pharmacology 2011, 11(suppl 1):p33.

AHU-377 Preparation Products And Raw materials

Raw materials

Preparation Products

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AHU-377 Suppliers

MedChemexpress LLC
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marketing@targetmol.com
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+86-13917743231
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sales@rrscientific.com
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United States
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View Lastest Price from AHU-377 manufacturers

BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
Product
Ahu377 149709-62-6
Price
US $0.00/g
Min. Order
1g
Purity
More Than 99%
Supply Ability
50kg/Month
Release date
2024-09-10
Henan Aochuang Chemical Co.,Ltd.
Product
AHU-377 149709-62-6
Price
US $0.00-0.00/KG
Min. Order
1KG
Purity
98%
Supply Ability
1ton
Release date
2022-09-29
Hong Kong Tiansheng New Material Trading Co., Ltd
Product
AHU-377 149709-62-6
Price
US $5.99/KG
Min. Order
1KG
Purity
99%
Supply Ability
100KG
Release date
2021-12-28

149709-62-6, AHU-377Related Search:


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