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KI0842Perindopril erbumine100 mg$272

Chemical Characteristic

Product NamePerindopril erbumine
SynonymsAceon
CAS No.107133-36-8
Molecular Weight 441.61
FormulaC23H43N3O5
Chemical Structure

Biological activities

Perindopril erbumine is angiotensin-converting enzyme (ACE) inhibitor. Perindopril erbumine has proven efficacy in a wide range of cardiovascular diseases. Perindopril erbumine is a prodrug that is hydrolyzed to its active metabolite, perindoprilat. [1] Long-term treatment with perindopril erbumine improves arterial compliance and increases the media-lumen ratio of peripheral resistance vessels. The active metabolite perindoprilat inhibits the ACE with an IC50 of 1.05 nM.[2] 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.[3] Perindopril erbumine (~2 µM) 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 in female BALB/c nude mice has a significant inhibitory effect on SCC-VII tumor growth. perindopril erbumine reduces blood vessel formation surrounding the tumors in vivo due to the suppression of VEGF-induced angiogenesis.[4]

Protocols

Perindopril erbumine is diluted in 100 mL of decarbonated water.[1]

References

[1] Hussein Al Ali SH, et al. Controlled release and angiotensin-converting enzyme inhibition properties of an antihypertensive drug based on a perindopril erbumine-layered double hydroxide nanocomposite. Int J Nanomedicine. 2012, 7: 2129-2141.
[2] Ceconi C, et al. Angiotensin-converting enzyme (ACE) inhibitors have different selectivity for bradykinin binding sites of human somatic ACE. Eur J Pharmacol. 2007, 577: 1-6. 閵嗏偓閵嗏偓
[3] Yoshiji H, et al. The angiotensin-I-converting enzyme inhibitor perindopril suppresses tumor growth and angiogenesis: possible role of the vascular endothelial growth factor. Clin Cancer Res. 2001, 7 (4): 1073-1078.
[4]Yasumatsu R, et al. 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, 130 (10): 567-573.

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