Ramipril

Catalog No.S1793

For research use only.

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

Ramipril  Chemical Structure

CAS No. 87333-19-5

Purity & Quality Control

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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 (from reference)

Cell Research:[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 Research:[4]
  • Animal Models: Male spontaneously hypertensive rats
  • Dosages: 0.03-10 mg/kg
  • Administration: Gavage, every day

Solubility (25°C)

In vitro

DMSO 83 mg/mL
(199.27 mM)
Water Insoluble
Ethanol '83 mg/mL

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+ 40% PEG 300+5% Tween 80+50% ddH2O
For best results, use promptly after mixing.

4.15 mg/mL

Chemical Information

Molecular Weight 416.51
Formula

C23H32N2O5

CAS No. 87333-19-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC(=O)C(CCC1=CC=CC=C1)NC(C)C(=O)N2C3CCCC3CC2C(=O)O

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03475186 Recruiting Drug: Ramipril Glioblastoma|Radiotherapy; Complications|Cognitive Decline|Chemoradiation Wake Forest University Health Sciences|National Cancer Institute (NCI) March 25 2019 Phase 2
NCT03440177 Recruiting Drug: Ramipril Obesity Morbid Norwegian University of Science and Technology|St. Olavs Hospital|Volvat Medisinsk Senter Stokkan|Namsos Hospital|Alesund Hospital January 2 2018 --
NCT01743014 Unknown status Drug: Ramipril|Drug: Clopidogrel Diabetes Type 2|Diabetic Nephropathy|Vascular Disease AHEPA University Hospital|Aristotle University Of Thessaloniki July 2012 Phase 4
NCT01829880 Unknown status -- Chronic Heart Failure|Cachexia The University Clinic of Pulmonary and Allergic Diseases Golnik October 2011 --
NCT01284621 Completed Drug: BI 10773|Drug: Ramipril Healthy Boehringer Ingelheim January 2011 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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