product name Enalapril Maleate
Description: Enalapril Maleate (also known as MK-421 Maleate) is an effective and potent nonsulfhydryl angiotensin-converting enzyme (ACE) inhibitor used in the treatment of hypertension, diabetic nephropathy, and chronic heart failure. Enalapril Maleate has been used to study diabetic angiopathy in diabetic rats and inhibition of ACE in hog plasma (I50=1.2nM). Enalapril treatment abolishes the deleterious effects of eNOS deficiency on blood pressure (BP), atherosclerosis, and kidney dysfunction in mice.
References: Clin Pharm. 1985;4(1):27-40; J Clin Invest. 2000;105(4):451-8; Pharmacol Res. 2011;64(5):482-92.
492.52
Formula
C20H28N2O5.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)
Solubility (In vivo)
Synonyms
MK-421 Maleate
other peoduct :
| 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. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Enalapril 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. |
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| References | Clin 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. |
