| Name | Perindopril erbumine |
| Description | Perindopril erbumine (S9490-3) is the tert-butylamine salt of perindopril, the ethyl ester of a non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Upon hydrolysis, Perindopril erbumine (S9490-3) 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. |
| In vitro | In rats with Alzheimer's disease, Perindopril Erbumine administered at a dosage of 1 mg/kg/day significantly inhibits hippocampal ACE activity, thereby preventing brain damage and cognitive impairments. When dosed at 3 mg/kg/day, it inhibits 6.4% of in vivo RAECs cell apoptosis (induced by lipopolysaccharides), in contrast to a 3.2% inhibition rate observed with ramipril. Perindopril Erbumine, at a dose of 2 mg/kg/day administered orally, markedly suppresses the growth of SCC-VII tumors by inhibiting VEGF-induced angiogenesis, reducing blood vessel formation around the tumor. Similarly, at 2 mg/kg/day, orally administered Perindopril Erbumine strongly inhibits the growth of BNL-HCC tumors in rats, an effect comparable to daily oral administration of 20 mg/kg, while a 20 mg/kg/day dosage of AT1-R antagonists losartan or candesartan shows no inhibitory effect. |
| In vivo | Perindopril Erbumine inhibits the conversion activities of mutated angiotensin-converting enzyme (ACE) (which contains two active sites) from angiotensin-I to angiotensin-II and from Aβ42 to Aβ40, with IC50 values of 0.03-0.1 μM and 0.01-0.03 μM, respectively. At a concentration of 2 μM, Perindopril Erbumine exhibits no significant cytotoxicity towards KB and SCC-VII cells, yet it reduces the production of angiotensin II and the transcription of VEGF in KB cells in a concentration-dependent manner. Compared to its binding affinity for the angiotensin-I binding site of ACE, Perindopril Erbumine has a higher affinity for the bradykinin binding site, with a bradykinin/angiotensin-I selectivity ratio of 1.44. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : 50 mg/mL (113.22 mM)
DMSO : 50 mg/mL (113.22 mM), Sonication is recommended.
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| Keywords | S 9490 | inhibit | Perindopril | S-9490 | Inhibitor | Perindopril tert-butylamine | Angiotensin-converting Enzyme (ACE) | S9490 | Perindopril erbumine | Apoptosis |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Captopril |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | NO PAINS Compound Library | FDA-Approved Drug Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
