Perindopril Erbumine

2 years -80 in solvent

Orally

A Phase III study to evaluate the efficacy and safety of a fixed-dose combination of Perindopril Arginine plus Amlodipine Besylate versus Perindopril Erbumine and Amlodipine Besylate in subjects with essential hypertension is currently recruiting participants.

Dissolved in DMSO, and diluted in saline

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 Abeta42-to-Abeta40-converting activity of mutated ACE containing two active domains (F-ACE) with IC50 of 0.03-0.1 uM, and 0.01-0.03 uM, respectively. [2] Perindopril Erbumine (ca.2 uM) 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]

ACE inhibitor binding assay, The binding assay is based on the competitive displacement of [125I]351A by Perindopril Erbumine and performed on whole endothelial cells. Subconfluent HUVECs in 6-well plates are rinsed with 2 mL binding buffer (140 mM NaCl, 2.7 mM KCl, 1.8 mM CaCl2, 1.03 mM MgCl2, 0.42 mM NaH2PO4, 10 mM HEPES, 2 mM sodium pyruvate, 5 mM glucose, pH 7.4), and the culture medium is replaced with 2.5 mL fresh binding buffer containing 5% fetal bovine serum (FBS). A set concentration of Perindopril Erbumine (2.5–12.5 uL, 0.1–50 nM) is added to the binding buffer. A saturating amount of [125I]351A (10 uL, typically 106 cpm) is then added to each sample and the plates are incubated at 37 C for 2 hours in a thermostatic bath. The cells are then rinsed twice with 1.5 mL binding buffer. Finally, the cells are extracted with 0.5 mL NaOH 1 N, incubated for 5 minutes, and the radioactivity is counted with a gamma counter. The radioactivity, which is due to [125I]351A binding, is inversely related to Pdopril Erbumine's affinity for endothelial ACE. The concentration of Perindopril Erbumine that displaces 50% of the bound radioligand is calculated from the competition curve.

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.