Ramipril

Catalog No.S1793 Batch:S179303

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Technical Data

Formula

C23H32N2O5
Molecular Weight 416.51 CAS No. 87333-19-5
Solubility (25°C)* In vitro DMSO 83 mg/mL (199.27 mM)
Ethanol 83 mg/mL (199.27 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.15mg/ml Taking the 1 mL working solution as an example, add 50 μL 83 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Ramipril(HOE-498) is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM.
Targets
ACE [1]
5 nM
In vitro

Ramipril is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM. [1] Ramipril enhances the activity of ACE-associated CK2 and the phosphorylation of ACE Ser1270 in cultured endothelial cells, but is unable to activate JNK or stimulate the nuclear accumulation of c-Jun in endothelial cells expressing a S1270A ACE mutant or in ACE-deficient cells. Prolonged Ramipril treatment increases ACE expression in primary cultures of human endothelial cells and in vivo (mouse lung), which can be prevented by pretreatment with the JNK inhibitor SP600125. [2] Ramipril displays little enhanced effect on the rate of in vitro endothelial apoptosis induced by the serum deprivation method. [3]
In vivo

Chronic in vivo administration of Ramipril to rats at a dosage that has similar hypotensive effects in vitro HUVECs significantly reduces the rate of LPS-induced apoptosis compared to the other ACE inhibitors, which contrasts with the apoptosis effect in vitro. [3] Ramipril inhibits systolic blood pressure (SBP) with IC50 of 1.97 mg/kg in spontaneously hypertensive rats (SHR). When in combination with AT1-receptor blockade by candesartan-cilexetil increases SBP reduction synergistically rather than additively. [4] Administration of Ramipril to spontaneously hypertensive rats (SHR) produces significant inhibition of aorta ACE and lung ACE with IC50 ~5 mg/kg, but shows little effect for brain ACE ex vivo. [5] Ramipril prevents beta cell dysfunction in osteoprotegerin treated mice through decreasing islet monocyte/macrophage infiltration, fibrosis and apoptosis involving decreasing RAS, growth factor genes and inflammatory molecules expressions. [6]
Features A pro-drug converted to its active metabolite, ramiprilat, by liver esterase enzymes.

Protocol (from reference)

Cell Assay:

[3]
  • Cell lines

    Human umbilical vein endothelial cells (HUVECs)

  • Concentrations

    ~1 μM

  • Incubation Time

    24 hours

  • Method

    The HUVECs are pretreated with the active metabolites of Ramipril for 24 hours. A serum deprivation method is used to induce apoptosis in the presence of Ramipril for an additional 24 hours. The rate of apoptosis is then determined using flow cytometry with two makers annexinV fluorescein isothiocyanate (FITC+) and propidium iodide (PI).
Animal Study:

[4]
  • Animal Models

    Male spontaneously hypertensive rats

  • Dosages

    0.03-10 mg/kg

  • Administration

    Gavage, every day

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.