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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:
产品名称
依那普利 二水合物, ≥98% (HPLC)
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)
Fredrik Palm et al.
Hypertension (Dallas, Tex. : 1979), 55(2), 298-304 (2010-01-06)
Angiotensin II maintains renal cortical blood flow and renal oxygenation in the clipped kidney of early 2-kidney, 1-clip Goldblatt hypertensive (2K,1C) rats. The involvement of Ang II is believed to decline, whereas oxidative stress increases during the progression of 2K,1C
Fabio Mangiacapra et al.
Journal of the American College of Cardiology, 61(6), 615-621 (2013-01-08)
This study investigated the influence of intracoronary enalaprilat on coronary microvascular function and peri-procedural outcome measures in patients with stable angina undergoing percutaneous coronary intervention (PCI). Intracoronary angiotensin-converting enzyme inhibitors have been shown to relieve myocardial ischemia in stable patients
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
Min Yu et al.
Molecules (Basel, Switzerland), 17(3), 2738-2751 (2012-03-08)
Enalaprilat (Ena.), an angiotensin II (Ang II) converting enzyme inhibitor (ACEI), can produce some therapeutic effects on hypertension, ventricular hypertrophy and myocardial remodeling in clinic, but its precise mechanism, especially its signaling pathways remain elusive. In this study, cardiac fibroblasts
Chinmoy Ghosh et al.
Drug testing and analysis, 4(2), 94-103 (2011-02-23)
A rapid and most sensitive method for simultaneous determination of enalapril (ENP) and its metabolite, enalaprilat (ENPT), in human plasma using ESI-LC-MS/MS (electrospray ionization liquid chromatography tandem mass spectrometry) positive ion multiple reactions monitoring (MRM) mode, was developed and validated.
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