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Merck
모든 사진(1)

문서

SML2064

Sigma-Aldrich

LBQ657

≥97% (HPLC)

동의어(들):

(2R,4S)-5-(Biphenyl-4-yl)-4-((3-carboxypropionyl)amino)-2-methylpentanoic acid, Desethyl sacubitril, Sacubitrilat

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About This Item

실험식(Hill 표기법):
C22H25NO5
CAS Number:
Molecular Weight:
383.44
MDL number:
UNSPSC 코드:
12352200
NACRES:
NA.77

분석

≥97% (HPLC)

형태

powder

광학 활성

[α]/D -35 to -27°, c = 1 in methanol

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

배송 상태

wet ice

저장 온도

−20°C

SMILES string

OC(CCC(N[C@H](CC1=CC=C(C2=CC=CC=C2)C=C1)C[C@H](C(O)=O)C)=O)=O

InChI

1S/C22H25NO5/c1-15(22(27)28)13-19(23-20(24)11-12-21(25)26)14-16-7-9-18(10-8-16)17-5-3-2-4-6-17/h2-10,15,19H,11-14H2,1H3,(H,23,24)(H,25,26)(H,27,28)/t15-,19+/m1/s1

InChI key

DOBNVUFHFMVMDB-BEFAXECRSA-N

생화학적/생리학적 작용

LBQ657 is the active metabolite of sacubitril. It is an inhibitor of the enkephalinase neprilysin (neutral endopeptidase, NEP) formed by the action of esterases on its prodrug sacubitril (AHU377), which is half of the heart failure combination drug Entresto, along with the angiotensin-receptor blocker Valsartan. LBQ657 prevents neprilysin′s degradation of atrial and brain natriuretic peptide, two blood pressure lowering peptides.

픽토그램

Health hazardExclamation mark

신호어

Danger

유해 및 위험 성명서

Hazard Classifications

STOT RE 1 - STOT SE 3

표적 기관

Bone,Kidney, Central nervous system

Storage Class Code

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

이미 열람한 고객

Imad Hanna et al.
Xenobiotica; the fate of foreign compounds in biological systems, 48(3), 300-313 (2017-03-11)
1. The potential for drug-drug interactions of LCZ696 (a novel, crystalline complex comprising sacubitril and valsartan) was investigated in vitro. 2. Sacubitril was shown to be a highly permeable P-glycoprotein (P-gp) substrate and was hydrolyzed to the active anionic metabolite LBQ657 by
Jessie Gu et al.
Journal of clinical pharmacology, 50(4), 401-414 (2009-11-26)
Angiotensin receptor blockade and neprilysin (NEP) inhibition together offer potential benefits for the treatment of hypertension and heart failure. LCZ696 is a novel single molecule comprising molecular moieties of valsartan and NEP inhibitor prodrug AHU377 (1:1 ratio). Oral administration of
Duncan J Campbell
Nature reviews. Cardiology, 14(3), 171-186 (2016-12-16)
Neprilysin has a major role in both the generation and degradation of bioactive peptides. LCZ696 (valsartan/sacubitril, Entresto), the first of the new ARNI (dual-acting angiotensin-receptor-neprilysin inhibitor) drug class, contains equimolar amounts of valsartan, an angiotensin-receptor blocker, and sacubitril, a prodrug
Sasha A S Kjeldsen et al.
Journal of the Endocrine Society, 5(9), bvab084-bvab084 (2021-08-03)
Inhibitors of the protease neprilysin (NEP) are used for treating heart failure, but are also linked to improvements in metabolism. NEP may cleave proglucagon-derived peptides, including the glucose and amino acid (AA)-regulating hormone glucagon. Studies investigating NEP inhibition on glucagon

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