84680-54-6 Usage
Description
Angiotensin-converting enzyme (ACE) converts angiotensin I to angiotensin II, a peptide hormone that impacts vascular smooth muscle tone and renal salt exchange, driving hypertension. Enalaprilat is the active metabolite of enalapril , an ACE inhibitor with roles in the management of hypertension, congestive heart failure, myocardial infarction, and diabetic nephropathies.. Enalaprilat is esterified with ethanol to produce enalapril in order to enable oral activity and subsequently metabolized in vivo to the active form by various esterases. Enalaprilat is reported to inhibit ACE activity with an IC50 value of 5.8 nM in vitro.
Chemical Properties
White Solid
Uses
Different sources of media describe the Uses of 84680-54-6 differently. You can refer to the following data:
1. Active metabolite of Enalapril. A nonsulfhydryl dipeptide angiotensin converting enzyme (ACE) inhibitor.
2. Active metabolite of Enalapril. A nonsulfhydryl dipeptide angiotensin converting enzyme (ACE) inhibitor. Enalapril EP Impurity C (Dihydrate).
Definition
ChEBI: The dihydrate form of enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor that is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients wi
h nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is administered by intravenous injection.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 84680-54-6 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 8,4,6,8 and 0 respectively; the second part has 2 digits, 5 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 84680-54:
(7*8)+(6*4)+(5*6)+(4*8)+(3*0)+(2*5)+(1*4)=156
156 % 10 = 6
So 84680-54-6 is a valid CAS Registry Number.
InChI:InChI=1/C18H24N2O5/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)/t12-,14+,15+/m0/s1
84680-54-6Relevant articles and documents
Method for the synthesis of amines and amino acids with organoboron derivatives
-
, (2008/06/13)
Amines and amino acids are prepared by reacting an amine, a carbonyl derivative, and an organoboron compound under mild conditions.
Prodrug derivatives of carboxylic acid drugs
-
, (2008/06/13)
Novel ester derivatives of carboxylic acid medicaments of formula (I), wherein R--COO--represents the acyloxy residue of a carboxylic acid drug or medicament, n is an integrer from 1 to 3, and R1 and R2 are the same or different and are selected from a group consisting of an alkyl, an alkenyl, an aryl, an aralkyl, a cycloalkyl and which group may be unsubstituted or substituted, or R1 and R2 together with the N forms a 4-, 5-, 6- or 7-membered heterocyclic ring, which in addition to the nitrogen atom may contain one or two further heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur and which heterocyclic group may be substituted. These compounds are highly biolabile prodrug forms of the corresponding carboxylic acid compounds and are highly susceptible to undergoing enzymatic hydrolysis in vivo whereas they are highly stable in aqueous solution. The novel derivatives are less irritating to mucosa than the parent carboxylic acids and may provide an improved bio-availability of the drugs.