Ramipril (Altace) is an angiotensin-converting enzyme (ACE) inhibitor with an IC50 of 5 nM. It is used to treat hypertension and congestive heart failure. ACE inhibitors lower the production of angiotensin II, therefore relaxing arterial muscles while at the same time enlarging the arteries, allowing the heart to pump blood more easily, and increasing blood flow due to more blood being pumped into and through larger passageways.
| Cell Experiment | |
|---|---|
| Cell lines | Human umbilical vein endothelial cells (HUVECs) |
| Preparation method | Pretreating the HUVECs with the active metabolites of Ramipril for 24 hours. Usinf a serum deprivation method to induce apoptosis in the presence of Ramipril for an additional 24 hours. Then determining the rate of apoptosis using flow cytometry with two makers annexinV fluorescein isothiocyanate (FITC+) and propidium iodide (PI). |
| Concentrations | ~1 μM |
| Incubation time | 24 hours |
| Animal Experiment | |
|---|---|
| Animal models | Male spontaneously hypertensive rats |
| Formulation | Dissolved in distilled water by using gum arabic (10% w/v) |
| Dosages | 0.03-10 mg/kg |
| Administration | Gavage, every day |
| Molecular Weight | 416.51 |
| Formula | C23H32N2O5 |
| CAS Number | 87333-19-5 |
| Solubility (25°C) | DMSO 80 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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