Home Endocrinology & Hormones RAAS inhibitor Perindopril Erbumine

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Perindopril Erbumine RAAS inhibitor

Cat.No.S1506

Perindopril Erbumine (S9490-3) is a pro-drug and metabolized in vivo by hydrolysis of the ester group to form Perindoprilat, the biologically active metabolite, a potent ACE inhibitor with IC50 of 1.05 nM. This compound is used for in vivo studies and Perindoprilat is recommened for in vitro research.
Perindopril Erbumine RAAS inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 441.6

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Chemical Information, Storage & Stability

Molecular Weight 441.6 Formula

C19H32N2O5.C4H11N

 Storage (From the date of receipt)
CAS No. 107133-36-8 Download SDF Storage of Stock Solutions

Synonyms S9490-3 Smiles CCCC(C(=O)OCC)NC(C)C(=O)N1C2CCCCC2CC1C(=O)O.CC(C)(C)N

Solubility

In vitro
Batch:

Ethanol : 88 mg/mL

Water : 30 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

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.

Mechanism of Action

Targets/IC50/Ki
ACE [1]
1.05 nM
In vitro
Perindopril Erbumine displays a higher binding affinity for the bradykinin binding sites than the angiotensin I binding sites of the angiotensin-converting enzyme (ACE) with bradykinin/angiotensin I selectivity ratio of 1.44. [1] This compound inhibits the angiotensin- and Aβ42-to-Aβ40-converting activity of mutated ACE containing two active domains (F-ACE) with IC50 of 0.03-0.1 μM, and 0.01-0.03 μM, respectively. [2] It (~2 μM) displays no significant cytotoxicity towards SCC-VII and KB cells, but can significantly reduce the production of angiotensin II and the transcription of VEGF in KB cells in a concentration-dependent manner. [3]
In vivo
Oral administration of Perindopril Erbumine at 2 mg/kg/day has a significant inhibitory effect on SCC-VII tumor growth, and reduces blood vessel formation surrounding the tumors in vivo due to the suppression of VEGF-induced angiogenesis. [3] Administration of this compound at 2 mg/kg/day displays a strong inhibitory effect of the BNL-HCC tumor growth in rats similar to that of 20 mg/kg/day and in contrast to the AT1-R antagonist candesartan or losartan which at the dose of 20 mg/kg/day has no inhibitory effect. [4] Administration of this chemical at 3 mg/kg/day significantly inhibits LPS-induced apoptosis by 6.4% in RAECs in vivo than that of ramipril by 3.2%. [5] Administration of this compound (1 mg/kg/day) significantly suppresses the hippocampal ACE activity, and prevents cognitive impairment and brain injury in rats with Alzheimer's disease (AD). [6]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/11309359/
  • [5] https://pubmed.ncbi.nlm.nih.gov/18004652/
  • [6] https://pubmed.ncbi.nlm.nih.gov/21593435/

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