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 Experiment | |
|---|---|
| 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 Experiment | |
|---|---|
| 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). |
| Dosages | 1 mg/kg |
| Administration | I.V. bolus |
| Molecular Weight | 348.4 |
| Formula | C18H24N2O5.2H2O |
| CAS Number | 84680-54-6 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| 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.
| Related ACE Products |
|---|
| Abz-Ser-Pro-3-nitro-Tyr
Abz-Ser-Pro-3-nitro-Tyr is the substrate of ACE2 (angiotensin-converting enzyme-2). |
| Temocaprilat
Temocaprilat (Temocapril diacid) is an inhibitor of angiotensin-converting enzyme (ACE). |
| FA-Phe-Phe
FA-Phe-Phe is a furylacryloyl (fa)-amino acid derivative, targeting to Angiotensin-converting Enzyme (ACE). |
| Garcinone B
Garcinone B, a xanthone derivative, is a nature product that could be isolated from the pericarp of Mangosteen. |
| Spirapril hydrochloride
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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