Ramipril

Catalog No.S1793

Ramipril  Chemical Structure

Molecular Weight(MW): 416.51

Ramipril is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM.

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In DMSO USD 130 In stock
USD 97 In stock
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Biological Activity

Description Ramipril is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM.
Features A pro-drug converted to its active metabolite, ramiprilat, by liver esterase enzymes.
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]

Protocol

Cell Research:[3]
+ Expand
  • 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).
    (Only for Reference)
Animal Research:[4]
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  • 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
    (Only for Reference)

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 individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/mL

* 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.

Chemical Information

Molecular Weight 416.51
Formula

C23H32N2O5

CAS No. 87333-19-5
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02924727 Recruiting Acute Myocardial Infarction Novartis Pharmaceuticals|Novartis December 2016 Phase 3
NCT02632747 Recruiting Diabetes Mellitus, Type 1 Boehringer Ingelheim|Eli Lilly and Company May 2016 Phase 2
NCT02791958 Recruiting Hypertension Ferrer Internacional S.A. March 2016 Phase 2
NCT02842424 Recruiting Peripheral Arterial Disease University of Nebraska October 2015 Phase 4
NCT02499822 Recruiting Hypertension|High Blood Pressure Variability Istituto Auxologico Italiano|Bayer October 2015 Phase 4
NCT02832973 Recruiting Hypertension Resistant to Conventional Therapy Sao Jose do Rio Preto University September 2015 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID