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      Enalapril Maleate (MK-421)
      Enalapril Maleate (MK-421)

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      This product is for research use only, not for human use. We do not sell to patients.
      Number： - + Pieces（InventoryPieces）
      InvivoChem Cat #: V1788
      CAS #: 76095-16-4 Purity ≥98%

      Description: Enalapril maleate (formerly MK-421; MK421; Glioten; Vasotec; Baripril; Renitec; Renitek), the maleate salt of enalapril, is a potent nonsulfhydryl angiotensin-converting enzyme (ACE) inhibitor widely 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.

      Related CAS#: 84680-54-6 (Enalaprilat Dihydrate); 75847-73-3 (Enalapril free base); 149404-21-7 (Enalapril sodium); 349554-02-5 (Enalapril D5 maleate); 690655-41-5 (NCX899, a NO-releasing derivative of enalapril)  

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      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)[[email protected]](CCC1=CC=CC=C1)N[[email protected]@H](C)C(=O)N2CCC[[email protected]]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;


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      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. 

      These protocols are for reference only. InvivoChem does not independently validate these methods.

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