推荐产品
方案
≥97% (HPLC)
表单
powder
旋光性
[α]/D -35 to -27°, c = 1 in methanol
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
运输
wet ice
储存温度
−20°C
SMILES字符串
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
生化/生理作用
LBQ657是sacubitril的活性代谢产物。它是一种通过酯酶对其前药沙必特（AHU377）的作用而形成的脑啡肽酶（中性内肽酶，NEP）抑制剂，是通过与血管紧张素受体阻滞剂缬沙坦组成的心力衰竭联合药物Entresto的另一半。LBQ657可阻止脑啡肽酶′对心房利钠和脑利钠肽这两种降血压肽的降解。
通过酯酶对其前药沙必特（AHU377）的作用而形成的脑啡肽酶（中性内肽酶，NEP）抑制剂
警示用语：
Danger
危险声明
危险分类
STOT RE 1 - STOT SE 3
靶器官
Bone,Kidney, Central nervous system
储存分类代码
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
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
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
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
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