84680-54-6, 76420-72-9 Enalaprilat dihydrate AKSci J55514
 
 
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  J55514    
Enalaprilat dihydrate
, 95%
 



IDENTITY
CAS Number:84680-54-6, 76420-72-9
MDL Number:MFCD00941393
MF:C18H24N2O5.2H2O
MW:384.43
EINECS:278-459-3
SPECIFICATIONS & PROPERTIES
Min. Purity Spec:95%
Physical Form (at 20°C):Solid
Melting Point:151-159°C
Long-Term Storage:Store long-term at -20°C
DOT/IATA TRANSPORT INFORMATION
Not hazardous material

BIOLOGICAL INFO
Solubility:DMSO: 70mg/mL; H2O: 5mg/mL; EtOH: 1mg/mL
Application(s):Angiotensin-converting enzyme (ACE) inhibitor; Antihypertensive Agent
Form:Hydrate

REVIEW

 'There are two isoforms of ACE: the somatic isoform, which exists as a glycoprotein comprised of a single polypeptide chain of 1277; and the testicular isoform, which has a lower molecular mass and is thought to play a role in sperm maturation and binding of sperm to the oviduct epithelium. Somatic ACE has two functionally active domains, N and C, which arise from tandem gene duplication. Although the two domains have high sequence similarity, they play distinct physiological roles. The C-domain is predominantly involved in blood pressure regulation while the N-domain plays a role in hematopoietic stem cell differentiation and proliferation. ACE inhibitors bind to and inhibit the activity of both domains, but have much greater affinity for and inhibitory activity against the C-domain. Enalaprilat, the principle active metabolite of enalapril, competes with ATI for binding to ACE and inhibits and enzymatic proteolysis of ATI to ATII. Decreasing ATII levels in the body decreases blood pressure by inhibiting the pressor effects of ATII as described in the Pharmacology section above. Enalapril also causes an increase in plasma renin activity likely due to a loss of feedback inhibition mediated by ATII on the release of renin and/or stimulation of reflex mechanisms via baroreceptors. Enalaprilat''s affinity for ACE is approximately 200,000 times greater than that of ATI and 300-1000 times greater than that enalapril. '

REFERENCES
[1]D.P. Ip and G.S. Brenner, in K. Florey (Editor), Analytical Profiles of Drug Substances, Vol. 16, Aca- demic Press, London, 1987, pp. 207-243.

GLOBALLY HARMONIZED SYSTEM (GHS)

Pictograms

Signal Word
Warning

Hazard Statements
H315; H319; H335

Precautionary Statements
P261; P264; P271; P280; P302+P352; P304+P340; P305+P351+P338; P312; P321; P332+P313; P337+P313; P362; P403+P233; P405; P501


RELATED PRODUCTS
H013Enalaprilat
X2108Enalaprilat dihydrate

Current as of October 2, 2022


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CATEGORIES

 APIs and Bioactives > ACE Inhibitors


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