Enalaprilat Dihydrate

Modify Date: 2024-01-05 22:10:20

Enalaprilat Dihydrate Structure
Enalaprilat Dihydrate structure
Common Name Enalaprilat Dihydrate
CAS Number 84680-54-6 Molecular Weight 384.424
Density N/A Boiling Point 563.5ºC at 760 mmHg
Molecular Formula C18H28N2O7 Melting Point 211-215°C
MSDS Chinese USA Flash Point 294.6ºC

 Use of Enalaprilat Dihydrate


Enalaprilat is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 1.94 nM.Target: ACEEnalaprilat has high affinity for human endothelial ACE with IC50 of 1.94 nM in vitro binding assay by displacing a saturating concentration of [125I]351A, a radiolabeled lisinopril analogue from ACE binding sites, and shows bradykinin/angiotensin I selectivity ratio of 1.00 calculated from double displacement experiments [1]. Enalaprilat attenuates the IGF-I induced neonatal rat cardiac fibroblast growth (30% reduction) in a concentration-dependent fashion, with IC50 of 90 mM [2].Administration of Enalaprilat induces a significant reduction of MAP at 70 minutes compared with the placebo group during haemorrhagic shock in rats, and results in a 50% reduction of CO, a general tendency of EB extravasation which is significant in the kidney and lungs, and a significant increase in ileal EB extravasation (53%) [3].

 Names

Name enalaprilat dihydrate
Synonym More Synonyms

 Enalaprilat Dihydrate Biological Activity

Description Enalaprilat is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 1.94 nM.Target: ACEEnalaprilat has high affinity for human endothelial ACE with IC50 of 1.94 nM in vitro binding assay by displacing a saturating concentration of [125I]351A, a radiolabeled lisinopril analogue from ACE binding sites, and shows bradykinin/angiotensin I selectivity ratio of 1.00 calculated from double displacement experiments [1]. Enalaprilat attenuates the IGF-I induced neonatal rat cardiac fibroblast growth (30% reduction) in a concentration-dependent fashion, with IC50 of 90 mM [2].Administration of Enalaprilat induces a significant reduction of MAP at 70 minutes compared with the placebo group during haemorrhagic shock in rats, and results in a 50% reduction of CO, a general tendency of EB extravasation which is significant in the kidney and lungs, and a significant increase in ileal EB extravasation (53%) [3].
Related Catalog
References

[1]. Ceconi, C., et al., Angiotensin-converting enzyme (ACE) inhibitors have different selectivity for bradykinin binding sites of human somatic ACE. Eur J Pharmacol, 2007. 577(1-3): p. 1-6.

[2]. van Eickels, M., H. Vetter, and C. Grohe, Angiotensin-converting enzyme (ACE) inhibition attenuates insulin-like growth factor-I (IGF-I) induced cardiac fibroblast proliferation. Br J Pharmacol, 2000. 131(8): p. 1592-6.

[3]. Schumacher, J., et al., Effects of candesartan and enalaprilat on the organ-specific microvascular permeability during haemorrhagic shock in rats. Br J Anaesth, 2006. 96(4): p. 437-43.

 Chemical & Physical Properties

Boiling Point 563.5ºC at 760 mmHg
Melting Point 211-215°C
Molecular Formula C18H28N2O7
Molecular Weight 384.424
Flash Point 294.6ºC
Exact Mass 384.189636
PSA 125.40000
LogP 1.32630
Index of Refraction 1.579
Storage condition -20°C Freezer

 Safety Information

Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Hazard Codes Xi
Risk Phrases R20/21/22:Harmful by inhalation, in contact with skin and if swallowed . R36/37/38:Irritating to eyes, respiratory system and skin .
Safety Phrases S22-S26-S36/37/39
RIDADR NONH for all modes of transport
RTECS TW3590600

 Articles5

More Articles
Evaluation of a rapid method for the therapeutic drug monitoring of aliskiren, enalapril and its active metabolite in plasma and urine by UHPLC-MS/MS.

J. Chromatogr. B. Analyt. Technol. Biomed. Life Sci. 980 , 79-87, (2015)

Given the increasing popularity of aliskiren, particularly in combination with angiotensin converting enzyme inhibitor (e.g. enalapril), it is important to determine whether its use in combination wit...

Role of multidrug resistance-associated protein 4 in the basolateral efflux of hepatically derived enalaprilat.

Drug Metab. Dispos. 42(9) , 1567-74, (2014)

Hepatic uptake and efflux transporters govern the systemic and hepatic exposure of many drugs and metabolites. Enalapril is a pharmacologically inactive prodrug of enalaprilat. Following oral administ...

Enalaprilat.

Dimens. Crit. Care Nurs. 19(2) , 22, (2000)

 Synonyms

MFCD00941393
ENALAPRILAT DIHYDRATE
2-[N-(1-Carboxy-3-phenylpropyl)alanyl]-1-pyrrolidinecarboxylic acid dihydrate
EINECS 278-459-3
1-Pyrrolidinecarboxylic acid, 2-[2-[(1-carboxy-3-phenylpropyl)amino]-1-oxopropyl]-, hydrate (1:2)