Perindopril Erbumine | CAS#107133-36-8 | 82834-16-0 | ACE Inhibitor

MedKoo Cat#: 318472 | Name: Perindopril Erbumine

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Perindopril Erbumine is an angiotensin-converting enzyme inhibitor. It is used in patients with hypertension and heart failure. Upon hydrolysis, perindopril erbumine is converted to its active form perindoprilat, inhibiting ACE and the conversion of angiotensin I to angiotensin II; consequently, angiotensin II-mediated vasoconstriction and angiotensin II-stimulated aldosterone secretion from the adrenal cortex are inhibited and diuresis and natriuresis ensue.

Chemical Structure

Perindopril Erbumine

CAS#107133-36-8 (erbumine)

Theoretical Analysis

MedKoo Cat#: 318472

Name: Perindopril Erbumine

CAS#: 107133-36-8 (erbumine)

Chemical Formula: C23H43N3O5

Exact Mass: 0.0000

Molecular Weight: 441.61

Elemental Analysis: C, 62.56; H, 9.81; N, 9.52; O, 18.12

Price and Availability

Size	Price	Availability
100mg	USD 175.00	2 Weeks
250mg	USD 300.00	2 Weeks
500mg	USD 500.00	2 Weeks
1g	USD 800.00	2 Weeks

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Related CAS #

107133-36-8 (Erbumine) 82834-16-0 (free base)

Synonym

Perindopril Erbumine; ACEON; Perindopril tert-butylamine; Perstarium; Pirindopril; S 9490; S 9490 3; S 9490-3; S 94903; S-9490.

IUPAC/Chemical Name

(2S,3aS,7aS)-1-[(2S)-2-[[(2S)-1-ethoxy-1-oxopentan-2-yl]amino]propanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carboxylic acid;2-methylpropan-2-amine

InChi Key

IYNMDWMQHSMDDE-MHXJNQAMSA-N

InChi Code

InChI=1S/C19H32N2O5.C4H11N/c1-4-8-14(19(25)26-5-2)20-12(3)17(22)21-15-10-7-6-9-13(15)11-16(21)18(23)24;1-4(2,3)5/h12-16,20H,4-11H2,1-3H3,(H,23,24);5H2,1-3H3/t12-,13-,14-,15-,16-;/m0./s1

SMILES Code

CCCC(C(=O)OCC)NC(C)C(=O)N1C2CCCCC2CC1C(=O)O.CC(C)(C)N

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Perindopril erbumine (Perindopril tert-butylamine salt) is a potent ACE inhibitor.

In vitro activity:

In the in vitro cell proliferation assays, there was no significant difference between the perindopril-treated group and the control group. However, the perindoprilat-treated group showed a significant reduction in mRNA expression of VEGF and inhibited the induction activity of the VEGF promoter in comparison to the control group. Perindoprilat treatment also significantly suppressed angiotensin II production in vitro. Reference: J Cancer Res Clin Oncol. 2004 Oct;130(10):567-73. https://pubmed.ncbi.nlm.nih.gov/15449186/

In vivo activity:

Perindopril, with significant inhibition of hippocampal ACE, significantly prevented cognitive impairment in this AD mouse model. This study next examined the protective effects of perindopril on cognitive impairment in PS2APP-transgenic mice overexpressing Aβ in the brain. Perindopril, without affecting brain Aβ deposition, significantly suppressed the increase in hippocampal ACE activity and improved cognition in PS2APP-transgenic mice, being associated with the suppression of hippocampal astrocyte activation and attenuation of superoxide. Reference: FASEB J. 2011 Sep;25(9):2911-20. https://pubmed.ncbi.nlm.nih.gov/21593435/

	Solvent	mg/mL	mM	comments
Solubility
	Water	50.0	113.22

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 441.61 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Yasumatsu R, Nakashima T, Masuda M, Ito A, Kuratomi Y, Nakagawa T, Komune S. Effects of the angiotensin-I converting enzyme inhibitor perindopril on tumor growth and angiogenesis in head and neck squamous cell carcinoma cells. J Cancer Res Clin Oncol. 2004 Oct;130(10):567-73. doi: 10.1007/s00432-004-0582-7. Epub 2004 Jul 27. PMID: 15449186. 2. Yoshiji H, Kuriyama S, Kawata M, Yoshii J, Ikenaka Y, Noguchi R, Nakatani T, Tsujinoue H, Fukui H. The angiotensin-I-converting enzyme inhibitor perindopril suppresses tumor growth and angiogenesis: possible role of the vascular endothelial growth factor. Clin Cancer Res. 2001 Apr;7(4):1073-8. PMID: 11309359. 3. Connolly K, Batacan R Jr, Jackson D, Vella R, Fenning A. Perindopril prevents development of obesity and hypertension in middle aged diet-induced obese rat models of metabolic syndrome. Life Sci. 2023 Feb 1;314:121291. doi: 10.1016/j.lfs.2022.121291. Epub 2022 Dec 16. PMID: 36535403. 4. Dong YF, Kataoka K, Tokutomi Y, Nako H, Nakamura T, Toyama K, Sueta D, Koibuchi N, Yamamoto E, Ogawa H, Kim-Mitsuyama S. Perindopril, a centrally active angiotensin-converting enzyme inhibitor, prevents cognitive impairment in mouse models of Alzheimer's disease. FASEB J. 2011 Sep;25(9):2911-20. doi: 10.1096/fj.11-182873. Epub 2011 May 18. PMID: 21593435.

In vitro protocol:

In vivo protocol:

1. Connolly K, Batacan R Jr, Jackson D, Vella R, Fenning A. Perindopril prevents development of obesity and hypertension in middle aged diet-induced obese rat models of metabolic syndrome. Life Sci. 2023 Feb 1;314:121291. doi: 10.1016/j.lfs.2022.121291. Epub 2022 Dec 16. PMID: 36535403. 2. Dong YF, Kataoka K, Tokutomi Y, Nako H, Nakamura T, Toyama K, Sueta D, Koibuchi N, Yamamoto E, Ogawa H, Kim-Mitsuyama S. Perindopril, a centrally active angiotensin-converting enzyme inhibitor, prevents cognitive impairment in mouse models of Alzheimer's disease. FASEB J. 2011 Sep;25(9):2911-20. doi: 10.1096/fj.11-182873. Epub 2011 May 18. PMID: 21593435.

1: Ďuriš M, Hradski J, Szucs R, Masár M. Microchip isotachophoresis for green and sustainable pharmaceutical quality control: Method validation and application to complex pharmaceutical formulations. J Chromatogr A. 2024 Aug 16;1729:465055. doi: 10.1016/j.chroma.2024.465055. Epub 2024 Jun 5. PMID: 38852265. 2: Jawed S, Cs S. Exploration of polymethacrylate and Hypromellose for the development of a non-sulfhydryl ACE inhibitor mucoadhesive system using Box- Behnken design: in-vitro and ex-vivo evaluation. Drug Dev Ind Pharm. 2023 Jan;49(1):115-128. doi: 10.1080/03639045.2023.2184636. Epub 2023 Mar 11. PMID: 36827197. 3: Wei X, Wang Y, Weng J, Lao Y, Deng R, Lu J, Yang S, Liu X. Combination of Perindopril Erbumine and Huangqi-Danshen Decoction Protects Against Chronic Kidney Disease via Sirtuin3/Mitochondrial Dynamics Pathway. Evid Based Complement Alternat Med. 2022 May 21;2022:5812105. doi: 10.1155/2022/5812105. PMID: 35677375; PMCID: PMC9170396. 4: Douroudgari H, Bahrami H, Valadi FM, Tozihi M, Najafloo N, Vahedpour M. Exploring and modeling the ion mobility spectrometry of perindopril: Example of protonation-dissociation reactions in large molecules. J Mass Spectrom. 2022 Mar;57(3):e4814. doi: 10.1002/jms.4814. PMID: 35233864. 5: Anwar S, Zaman M, Raja MAG, Mahmood A, Amjad MW. Rosuvastatin, Perindopril and Ezetimibe loaded instant release buccal films: Development and in vitro characterization. J Appl Biomed. 2020 Dec;18(4):115-125. doi: 10.32725/jab.2020.015. Epub 2020 Oct 27. PMID: 34907764. 6: Liu X, Deng R, Wei X, Wang Y, Weng J, Lao Y, Lu J, Xiong G, Li S. Jian-Pi-Yi- Shen formula enhances perindopril inhibition of chronic kidney disease progression by activation of SIRT3, modulation of mitochondrial dynamics, and antioxidant effects. Biosci Rep. 2021 Oct 29;41(10):BSR20211598. doi: 10.1042/BSR20211598. PMID: 34633033; PMCID: PMC8536834. 7: Ijaz H, Tulain UR, Azam F, Qureshi J. Thiolation of arabinoxylan and its application in the fabrication of pH-sensitive thiolated arabinoxylan grafted acrylic acid copolymer. Drug Dev Ind Pharm. 2019 May;45(5):754-766. doi: 10.1080/03639045.2019.1569041. Epub 2019 Feb 11. PMID: 30640559. 8: Luu E, Ita KB, Morra MJ, Popova IE. The Influence of Microneedles on the Percutaneous Penetration of Selected Antihypertensive Agents: Diltiazem Hydrochloride and Perindopril Erbumine. Curr Drug Deliv. 2018;15(10):1449-1458. doi: 10.2174/1567201815666180730125941. PMID: 30058488; PMCID: PMC6340158. 9: Elliott WJ, Bistrika EA. Perindopril arginine and amlodipine besylate for hypertension: a safety evaluation. Expert Opin Drug Saf. 2018 Feb;17(2):207-216. doi: 10.1080/14740338.2018.1397129. Epub 2017 Oct 31. PMID: 29065722. 10: Buda V, Andor M, Ledeti A, Ledeti I, Vlase G, Vlase T, Cristescu C, Voicu M, Suciu L, Tomescu MC. Comparative Solid-State Stability of Perindopril Active Substance vs. Pharmaceutical Formulation. Int J Mol Sci. 2017 Jan 15;18(1):164. doi: 10.3390/ijms18010164. PMID: 28098840; PMCID: PMC5297797. 11: Ölçer A, Ölçer M, İnce I, Karasulu E. The advantages of combination therapy on hypertension: development of immediate release perindopril-indapamide tablet and assessment of bioequivalence studies. Pharm Dev Technol. 2016 Mar;21(2):239-49. doi: 10.3109/10837450.2014.991878. Epub 2015 Oct 13. PMID: 26794937. 12: Fael H, Sakur AA. Novel Spectrofluorimetric Method for the Determination of Perindopril Erbumine Based on Fluorescence Quenching of Rhodamine B. J Fluoresc. 2015 Nov;25(6):1577-84. doi: 10.1007/s10895-015-1666-2. Epub 2015 Oct 5. PMID: 26438658. 13: Elliott WJ. Perindopril arginine + amlodipine for the treatment of hypertension in the USA. Expert Opin Pharmacother. 2015;16(14):2217-29. doi: 10.1517/14656566.2015.1083978. Epub 2015 Sep 1. PMID: 26325023. 14: Fael H, Sakur AA. Novel Spectrofluorimetric Method for the Determination of Perindopril Erbumine Based on Charge Transfer Reaction with 7-Hydroxycoumarin. J Fluoresc. 2015 Jul;25(4):811-8. doi: 10.1007/s10895-015-1596-z. Epub 2015 Jul 7. PMID: 26149499. 15: Elliott WJ, Whitmore J, Feldstein JD, Bakris GL. Efficacy and safety of perindopril arginine + amlodipine in hypertension. J Am Soc Hypertens. 2015 Apr;9(4):266-74. doi: 10.1016/j.jash.2015.01.012. Epub 2015 Jan 29. PMID: 25804495. 16: Ölçer M, Ölçer A, İnce İ, Karasulu E. Development and in vitro/in vivo evaluation of immediate release perindopril tablets. Pharm Dev Technol. 2015;20(6):684-93. doi: 10.3109/10837450.2014.915568. Epub 2014 May 6. PMID: 24799074. 17: Helal F, Lane ME. Transdermal delivery of Angiotensin Converting Enzyme inhibitors. Eur J Pharm Biopharm. 2014 Sep;88(1):1-7. doi: 10.1016/j.ejpb.2014.03.007. Epub 2014 Mar 20. PMID: 24657822. 18: Dugga HH, Peraman R, Nayakanti D. Stability-indicating RP-HPLC method for the quantitative analysis of perindopril erbumine in tablet dosage form. J Chromatogr Sci. 2014 Apr;52(4):315-20. doi: 10.1093/chromsci/bmt031. Epub 2013 May 19. PMID: 23690066. 19: Vehovec T, Gartner A, Planinšek O, Obreza A. Influence of different types of commercially available microcrystalline cellulose on degradation of perindopril erbumine and enalapril maleate in binary mixtures. Acta Pharm. 2012 Dec;62(4):515-28. doi: 10.2478/v10007-012-0039-5. PMID: 23333887. 20: Hussein Al Ali SH, Al-Qubaisi M, Hussein MZ, Ismail M, Zainal Z, Hakim MN. Comparative study of Mg/Al- and Zn/Al-layered double hydroxide-perindopril erbumine nanocomposites for inhibition of angiotensin-converting enzyme. Int J Nanomedicine. 2012;7:4251-62. doi: 10.2147/IJN.S32267. Epub 2012 Aug 3. PMID: 22904631; PMCID: PMC3418079.