Home Endocrinology & Hormones RAAS inhibitor Perindopril Erbumine For research use only.

Perindopril Erbumine

Synonyms: S9490-3

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. Perindopril Erbumine is used for in vivo studies and Perindoprilat is recommened for in vitro research.

Perindopril Erbumine Chemical Structure

Perindopril Erbumine Chemical Structure

CAS: 107133-36-8

Selleck's Perindopril Erbumine has been cited by 1 publication

Purity & Quality Control

Batch: Purity: 99.99%
99.99

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Biological Activity

Description 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. Perindopril Erbumine is used for in vivo studies and Perindoprilat is recommened for in vitro research.
Targets
ACE [1]
1.05 nM
In vitro
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] Perindopril Erbumine 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] Perindopril Erbumine (~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
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 Perindopril Erbumine 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 Perindopril Erbumine 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 Perindopril Erbumine (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]
Animal Research Animal Models Female BALB/c nude mice injected with SCC-VII cells
Dosages 1 or 2 mg/kg/day
Administration Orally

Chemical lnformation & Solubility

Molecular Weight 441.6 Formula

C19H32N2O5.C4H11N
CAS No. 107133-36-8 SDF Download Perindopril Erbumine SDF
Smiles CCCC(C(=O)OCC)NC(C)C(=O)N1C2CCCCC2CC1C(=O)O.CC(C)(C)N
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 88 mg/mL

Water : 30 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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In vivo
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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.
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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.

Handling Instructions

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