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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
50 mg | $30 | In Stock | |
100 mg | $41 | In Stock | |
200 mg | $63 | In Stock | |
500 mg | $98 | In Stock | |
1 g | $153 | In Stock | |
1 mL x 10 mM (in DMSO) | $39 | In Stock |
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. |
Targets&IC50 | ACE:1.05 nM |
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. |
Alias | S9490-3, Perindopril tert-butylamine salt |
Molecular Weight | 441.61 |
Formula | C23H43N3O5 |
Cas No. | 107133-36-8 |
Smiles | CC(C)(C)N.N1([C@@H]2[C@H](C[C@H]1C(=O)O)CCCC2)C(=O)[C@@H](N[C@H](C(=O)OCC)CCC)C |
Relative Density. | 1.15 g/cm3 |
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. ![]() | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
H2O/DMSO
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