E9658
依那普利 二水合物
≥98% (HPLC)
别名:
(2S)-1-[(2S)-2-[[(1S)-1-Carboxy-3-phenyl-propyl]amino]propanoyl]pyrrolidine-2-carboxylic acid, Vasotec
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关于此项目
经验公式（希尔记法）:
C18H24N2O5 ·2H2O
化学文摘社编号:
分子量:
384.42
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
EC Number:
278-459-3
MDL number:
Assay:
≥98% (HPLC)
Quality level:
InChI key
MZYVOFLIPYDBGD-MLZQUWKJSA-N
InChI
1S/C18H24N2O5.2H2O/c1-12(16(21)20-11-5-8-15(20)18(24)25)19-14(17(22)23)10-9-13-6-3-2-4-7-13;;/h2-4,6-7,12,14-15,19H,5,8-11H2,1H3,(H,22,23)(H,24,25);2*1H2/t12-,14-,15-;;/m0../s1
SMILES string
O.O.C[C@H](N[C@@H](CCc1ccccc1)C(O)=O)C(=O)N2CCC[C@H]2C(O)=O
assay
≥98% (HPLC)
solubility
H2O: 14 mg/mL at 60 °C (warming for 5 minutes), DMSO: 64 mg/mL
originator
Merck & Co., Inc., Kenilworth, NJ, U.S.
storage temp.
room temp
Quality Level
Gene Information
human ... ACE(1636)
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相关类别
Biochem/physiol Actions
Enalapril, the ethyl ester of enalaprilat exhibits slight pharmacological activity until it is hydrolyzed in the liver to enalaprilat. Enalaprilat, a IV form of an angiotensin-converting-enzyme inhibitor (ACE) prevents the transformation of angiotensin I to angiotensin II, a potent vasoconstrictor.
Enalaprilat is an inhibitor of angiotensin converting enzyme (ACE), antihypertensive, and a Bradykinin B1 receptor activator.
Enalaprilat is an inhibitor of angiotensin converting enzyme (ACE), antihypertensive, and a Bradykinin B1 receptor activator. Enalaprilat has nM potency versus ACE and also activates B1 receptors to release NO.
Features and Benefits
This compound is featured on the Angiotensin Receptors and Bradykinin Receptors pages of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by Merck & Co., Inc., Kenilworth, NJ, U.S.. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
P F O'Tierney et al.
American journal of physiology. Regulatory, integrative and comparative physiology, 299(2), R573-R578 (2010-05-21)
The fetal heart is highly sensitive to changes in mechanical load. We have previously demonstrated that increased cardiac load can stimulate cell cycle activity and maturation of immature cardiomyocytes, but the effects of reduced load are not known. Sixteen fetal
Jiandong Zhang et al.
American journal of physiology. Renal physiology, 301(4), F723-F732 (2011-07-29)
The limited antifibrotic effect of therapeutic angiotensin blockade, the fact that angiotensin blockade dramatically elevates renin levels, and recent evidence that renin has an angiotensin-independent, receptor-mediated profibrotic action led us to hypothesize that combining renin receptor inhibition and ANG II
Gérémy Abdull Koumbadinga et al.
Peptides, 31(8), 1546-1554 (2010-05-11)
Angiotensin converting enzyme (ACE) is a drug target and an effective bradykinin (BK)-inactivating ectopeptidase. We exploited a recently described [(3)H]enalaprilat binding assay to quantify the full dynamic range of ACE expression in intact human umbilical vein endothelial cells (HUVECs) stimulated
Diamantino Ribeiro Salgado et al.
Shock (Augusta, Ga.), 35(6), 542-549 (2011-02-02)
Severe sepsis is frequently associated with microcirculatory abnormalities despite seemingly adequate hemodynamic resuscitation. As increased serum angiotensin II levels may play a role in this dysfunction, we evaluated the microcirculatory effects of enalaprilat in an experimental model of septic shock.
Vanessa Fontana et al.
Cardiovascular drugs and therapy, 26(6), 511-519 (2012-10-23)
Angiotensin-converting enzyme inhibitors (ACEi) may downregulate matrix metalloproteinases (MMPs). We examined whether enalapril affects MMP-2, MMP-8, and MMP-9 levels and activity, and their endogenous inhibitors (tissue inhibitors of MMPs, TIMP-1 and TIMP-2) levels in hypertensive patients. Moreover, we assessed the
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