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Enalapril Maleate(MK-421)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Enalapril Maleate(MK-421)图片
CAS NO:76095-16-4
规格:≥98%
包装与价格:
包装价格(元)
250mg电议
500mg电议
1g电议
2g电议
5g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)492.52
FormulaC20H28N2O5.C4H4O4
CAS No.76095-16-4
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 99 mg/mL (201.0 mM)
Water: <1 mg/mL
Ethanol: 4 mg/mL (8.1 mM)
Other infoChemical Name: (Z)-but-2-enedioic acid;(2S)-1-[(2S)-2-[[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]propanoyl]pyrrolidine-2-carboxylic acid
InChi Key: OYFJQPXVCSSHAI-QFPUQLAESA-N
InChi Code: InChI=1S/C20H28N2O5.C4H4O4/c1-3-27-20(26)16(12-11-15-8-5-4-6-9-15)21-14(2)18(23)22-13-7-10-17(22)19(24)25;5-3(6)1-2-4(7)8/h4-6,8-9,14,16-17,21H,3,7,10-13H2,1-2H3,(H,24,25);1-2H,(H,5,6)(H,7,8)/b;2-1-/t14-,16-,17-;/m0./s1
SMILES Code: CCOC(=O)[C@H](CCC1=CC=CC=C1)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)O.C(=C\C(=O)O)\C(=O)O
SynonymsMK-421 Maleate; Glioten; Vasotec; Baripril; Maleate, Enalapril; MK 421; MK-421; MK421; Renitec; Renitek;
实验参考方法
In Vitro

In vitro activity: Enalapril is rapidly converted by ester hydrolysis to enalaprilat, a potent ACE inhibitor; Enalapril itself is only a weak ACE inhibitor. Enalapril lowers peripheral vascular resistance without causing an increase in heart rate.

In VivoEnalapril treatment abolishes the deleterious effects of eNOS deficiency on blood pressure (BP), atherosclerosis, and kidney dysfunction in nnee mice. Enalapril causes a dose-dependent increase in fore limb strength in the mdx mouse. Enalapril causes a dose-dependent reduction of superoxide anion production in tibialis anterior muscle of the mdx mouse as observed by dihydroethidium staining. Enalapril (5 mg/kg) reduces the area of muscle necrosis in both gastrocnemious muscle and diaphragm, without significant effect on non-muscle area. Enalapril Maleate results in significant increases in kidney weight and in concentrations of urinary albumin, N-acetyl-fl-d-glucosamidase (NAG) and serum ET-1 in streptozotocin (STZ)-induced diabetic (STZ-DM) rats as compared with the non-diabetic rats, and the concentration of ET-1 in the kidneys tended to be increased. Enalapril Maleate results in increased mesangial cell proliferation, matrix expansion and enlarged mesangial area in the kidney of the diabetic rats. Enalapril Maleate reduces increased concentrations of urinary albumin and NAG in the STZ-DM rats to the control values with a slight improvement in the electron microscopic changes.
Animal model Rats
Formulation & Dosage oral
ReferencesClin Pharm. 1985 Jan-Feb;4(1):27-40; J Clin Invest. 2000 Feb;105(4):451-8; Pharmacol Res. 2011 Nov;64(5):482-92.