Home Endocrinology & Hormones RAAS inhibitor - ACE inhibitor Ramipril For research use only.

Ramipril

Synonyms: HOE-498

Ramipril(HOE-498) is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM.

Ramipril Chemical Structure

Ramipril Chemical Structure

CAS: 87333-19-5

Purity & Quality Control

Batch: Purity: 100%
100

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Description Ramipril(HOE-498) 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
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]
Cell Research 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).
In Vivo
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]
Animal Research Animal Models Male spontaneously hypertensive rats
Dosages 0.03-10 mg/kg
Administration Gavage, every day
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05438316 Completed Bioequivalence Pharmtechnology LLC|Ligand Research LLC June 17 2022 Phase 1
NCT03475186 Recruiting Glioblastoma|Radiotherapy; Complications|Cognitive Decline|Chemoradiation Wake Forest University Health Sciences|National Cancer Institute (NCI) March 25 2019 Phase 2
NCT03440177 Recruiting 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 Diabetes Type 2|Diabetic Nephropathy|Vascular Disease AHEPA University Hospital|Aristotle University Of Thessaloniki July 2012 Phase 4

Chemical lnformation & Solubility

Molecular Weight 416.51 Formula

C23H32N2O5
CAS No. 87333-19-5 SDF Download Ramipril SDF
Smiles CCOC(=O)C(CCC1=CC=CC=C1)NC(C)C(=O)N2C3CCCC3CC2C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 83 mg/mL ( (199.27 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 83 mg/mL

Water : Insoluble


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In vivo
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