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Ramipril RAAS inhibitor

Name: Ramipril
Brand: Selleck Chemicals
SKU: S1793
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S1793

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

Chemical Structure

Molecular Weight: 416.51

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.46%

99.46

Related Targets	Adrenergic Receptor Estrogen/progestogen Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE Opioid Receptor THR PGES Aromatase 5-alpha Reductase CCK receptor Mineralocorticoid Receptor GHSR SSTR TSH Receptor GNRH Receptor PGDS
Related Products	Temocapril HCl

Chemical Information, Storage & Stability

Molecular Weight	416.51	Formula	C₂₃H₃₂N₂O₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	87333-19-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	HOE-498			Smiles	CCOC(=O)C(CCC1=CC=CC=C1)NC(C)C(=O)N2C3CCCC3CC2C(=O)O

Solubility

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.150mg/ml (9.96mM)	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.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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.

Mechanism of Action

Features	A pro-drug converted to its active metabolite, ramiprilat, by liver esterase enzymes.
Targets/IC₅₀/Ki	ACE ^[1] 5 nM
In vitro	Ramipril is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM. ^[1] This compound 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 treatment with this chemical 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] It 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] This compound 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 this chemical 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] This agent 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]
References	https://pubmed.ncbi.nlm.nih.gov/2905962/ https://pubmed.ncbi.nlm.nih.gov/14615289/ https://pubmed.ncbi.nlm.nih.gov/18004652/ https://pubmed.ncbi.nlm.nih.gov/15076168/ https://pubmed.ncbi.nlm.nih.gov/2557876/ https://pubmed.ncbi.nlm.nih.gov/20832449/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05438316	Completed	Bioequivalence	Pharmtechnology LLC\|Ligand Research LLC	June 17 2022	Phase 1
NCT03475186	Active not 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

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