Enalaprilat dihydrate_product_DataBase

Bioactivity

Enalaprilat dihydrate (MK-422), the active metabolite of the oral prodrug Enalapril, is a potent, competitive and long-acting angiotensin-converting enzyme (ACE) inhibitor, with an IC50 of 1.94 nM. Enalaprilat dihydrate can be used for the research of hypertension[1][2][3].

Target

IC50: 1.94 nM (ACE)

Invitro

Enalaprilat (1 nM-10 μM; 24 h) dihydrate attenuates the IGF-I induced neonatal rat cardiac fibroblast growth (30% reduction) in a concentration-dependent fashion, with an IC50 of 90 mM[2].

In Vivo

Enalaprilat (0.01%-2.9% in the eyedrop solution) dihydrate shows significant intraocular pressure (IOP)-lowering effect in rabbits[3].

Name

Enalaprilat dihydrate

CAS

84680-54-6

Formula

C18H28N2O7

Molar Mass

384.42

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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 Dec 22;577(1-3):1-6. [2]. Eickels M, et, al. Angiotensin-converting enzyme (ACE) inhibition attenuates insulin-like growth factor-I (IGF-I) induced cardiac fibroblast proliferation. Br J Pharmacol. 2000 Dec;131(8):1592-6. [3]. Loftsson T, et, al. Enalaprilat and enalapril maleate eyedrops lower intraocular pressure in rabbits. Acta Ophthalmol. 2010 May;88(3):337-41.

PeptideDB

Enalaprilat dihydrate

CAS: 84680-54-6 F: C18H28N2O7 W: 384.42