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    Perindopril Erbumine (S-9490-3)
    Perindopril Erbumine (S-9490-3)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1782
    CAS #: 107133-36-8 Purity ≥98%

    Description: Perindopril Erbumine (also called S9490-3; Pirindopril; ACEON; Perindopril tert-butylamine; Perstarium), the tert-butylamine salt of perindopril, is a long acting and brain penetrant ACE (angiotensin-converting enzyme) inhibitor with anti-hypertensive effects. It inhibits ACE with an IC50 of 1.05 nM and has been approved for use in the treatment of hypertension and heart failure. Perindopril Erbumine can suppress the increase in hippocampal ACE activity and improves cognition in PS2APP-transgenic mice. Perindopril Erbumine displays a higher binding affinity for the bradykinin binding sites than the angiotensin I binding sites of ACE. 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.

    References: Eur J Pharmacol. 2007 Dec 22;577(1-3):1-6; J Biol Chem. 2009 Nov 13;284(46):31914-20.

    Related CAS #: 82834-16-0 (free base)  107133-36-8 (Erbumine salt) 

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    Molecular Weight (MW)441.6 
    FormulaC19H32N2O5.C4H11N 
    CAS No.107133-36-8 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: <1 mg/mL 
    Water: 88 mg/mL (199.3 mM)
    Ethanol: 88 mg/mL (199.3 mM)
    Solubility (In vivo)Saline: 30 mg/mL 
    SynonymsS 9490; S-9490; Pirindopril; S9490; S 9490-3; S9490-3; ACEON; Perindopril tert-butylamine; Perstarium; S 9490 3; S 94903.


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    In Vitro

    In vitro activity: 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. 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. 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.


    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. 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. 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%. 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). 
    Animal modelFemale BALB/c nude mice injected with SCC-VII cells 
    Formulation & DosageDissolved in DMSO, and diluted in saline; 1 or 2 mg/kg/day; p.o.
    References

    Eur J Pharmacol. 2007 Dec 22;577(1-3):1-6; J Biol Chem. 2009 Nov 13;284(46):31914-20; J Cancer Res Clin Oncol. 2004 Oct;130(10):567-73. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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