Enalaprilat dihydrate is the first dicarboxylate-containing ACE inhibitor with an IC50 of 4 nM. It was developed partly to overcome these limitations of captopril. The sulfhydryl-moiety was replaced by a carboxylate-moiety, but additional modifications were required in its structure-based design to achieve a similar potency to captopril.
Biomedicines. 2023 May 30;11(6):1581.
Learning and Investigation of the Role of Angiotensin-Converting Enzyme in Radiotherapy for Nasopharyngeal Carcinoma
Enalaprilat Dihydrate purchased from AbMole
|Cell lines||Rat cardiac fibroblasts cell lines|
|Preparation method||After 24 hours incubation in serum-free medium (DMEM), stimulating cells with IGF-I (1-100 nM) and coincubating with Enalaprilat (1 nM-10 μM) for 24 hours. Using a colorimetric immunoassay during the last 4 hours of the 24 hours incubation period to assesse cellular proliferation by 5-bromo-2'-deoxyuridine (BrdU) incorporation . Mearsuring the extinctions at 450 nm in an ELISA plate reader. All values consist of an n=9.|
|Concentrations||Dissolved in DMSO, final concentrations 1 nM - 10 μM|
|Incubation time||24 hours|
|Animal models||Male Sprague–Dawley rats|
|Formulation||Dissolved in a vehicle solution (1 mg in 950 μL of phosphate buffered saline and 50 μL 1M Na2CO3).|
|Solubility (25°C)||DMSO 60 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Gabriel R Estrela, et al. Front Mol Biosci. Angiotensin-Converting Enzyme Inhibitor Protects Against Cisplatin Nephrotoxicity by Modulating Kinin B1 Receptor Expression and Aminopeptidase P Activity in Mice
|Related ACE Products|
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Garcinone B, a xanthone derivative, is a nature product that could be isolated from the pericarp of Mangosteen.
Spirapril (SCH 33844) hydrochloride is a potent angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril competitively binds to ACE and prevents the conversion of angiotensin I to angiotensin II. Spirapril is an orally active proagent of Spiraprilat and can be used for the research of hypertension, congestive heart failure.
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