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Ramipril

Cat. No. M3506
Ramipril Structure
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100mg USD 60  USD60 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
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
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Barbara Toffoli, et al. Mol Cell Endocrinol. Osteoprotegerin induces morphological and functional alterations in mouse pancreatic islets

[2] C Ceconi, et al. Cardiovasc Drugs Ther. Differences in the effect of angiotensin-converting enzyme inhibitors on the rate of endothelial cell apoptosis: in vitro and in vivo studies

[3] Walter Raasch, et al. J Hypertens. Combined blockade of AT1-receptors and ACE synergistically potentiates antihypertensive effects in SHR

[4] D W Cushman, et al. Br J Clin Pharmacol. Comparisons in vitro, ex vivo, and in vivo of the actions of seven structurally diverse inhibitors of angiotensin converting enzyme (ACE)

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Keywords: Ramipril supplier, ACE, inhibitors, activators


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