[CAS NO. 107133-36-8] Perindopril Erbumine

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PRODUCTS SPECIFICATIONS [107133-36-8]

Catalog

SLK-S1506

Brand

Selleck

CAS

107133-36-8

DESCRIPTION [107133-36-8]

Overview

MDL	MFCD02313824
Molecular Weight	441.6
Molecular Formula	C19H32N2O5.C4H11N
SMILES	C(C)(C)(C)N.C([C@@H](N[C@H](C(OCC)=O)CCC)C)(=O)N1[C@@]2([C@](C[C@H]1C(O)=O)(CCCC2)[H])[H]

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.2645 mL	11.3225 mL	22.6449 mL
5 mM	0.4529 mL	2.2645 mL	4.5290 mL
10 mM	0.2264 mL	1.1322 mL	2.2645 mL
50 mM	0.0453 mL	0.2264 mL	0.4529 mL

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 inhibitor with 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

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).

References

[1] Ceconi C, et al. Eur J Pharmacol, 2007, 577(1-3), 1-6.
[2] Zou K, et al. J Biol Chem, 2009, 284(46), 31914-31920.
[3] Yasumatsu R, et al. J Cancer Res Clin Oncol, 2004, 130(10), 567-573.
[4] Yoshiji H, et al. Clin Cancer Res, 2001, 7(4), 1073-1078.
[5] Ceconi C, et al. Cardiovasc Drugs Ther, 2007, 21(6), 423-429.
[6] Dong YF, et al. FASEB J, 2011, 25(9), 2911-2920.

Synonyms

1H-Indole-2-carboxylic acid, 1-[(2S)-2-[[(1S)-1-(ethoxycarbonyl)butyl]amino]-1-oxopropyl]octahydro-, (2S,3aS,7aS)-, compd. with 2-methyl-2-propanamine (1:1)

1H-Indole-2-carboxylic acid, 1-[2-[[1-(ethoxycarbonyl)butyl]amino]-1-oxopropyl]octahydro-, [2S-[1[R*(R*)],2α,3aβ,7aβ]]-, compd. with 2-methyl-2-propanamine (1:1)

2-Propanamine, 2-methyl-, [2S-[1[R*(R*)],2α,3aβ,7aβ]]-1-[2-[[1-(ethoxycarbonyl)butyl]amino]-1-oxopropyl]octahydro-1H-indole-2-carboxylate

2-Propanamine, 2-methyl-, (2S,3aS,7aS)-1-[(2S)-2-[[(1S)-1-(ethoxycarbonyl)butyl]amino]-1-oxopropyl]octahydro-1H-indole-2-carboxylate

S 9490-3

McN-A 2833-109

Perindopril erbumine

Perindopril-tert-butylamine

Butylaminiperindopril

Prestarium

Coversyl

Coversum

Aceon

Perinodpril erbimune

Procaptan

Perindopril tert-butylamine salt

Perinodopril

Perigard

Conversyl

Perindopril tert-butylamine