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Perindopril erbumine

Catalog No. T1484L   CAS 107133-36-8
Synonyms: S9490-3, Perindopril tert-butylamine salt

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.

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Perindopril erbumine Chemical Structure
Perindopril erbumine, CAS 107133-36-8
Pack Size Availability Price/USD Quantity
50 mg In stock $ 38.00
100 mg In stock $ 52.00
200 mg In stock $ 78.00
500 mg In stock $ 126.00
1 mL * 10 mM (in DMSO) In stock $ 39.00
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Purity: 99.8%
Purity: 99.75%
Purity: 99.23%
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Biological Description
Chemical Properties
Storage & Solubility Information
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.
Synonyms S9490-3, Perindopril tert-butylamine salt
Molecular Weight 441.61
Formula C23H43N3O5
CAS No. 107133-36-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 50 mg/mL (113.22 mM)

DMSO: 10 mg/mL (22.64 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Ceconi C, et al. Eur J Pharmacol, 2007, 577(1-3), 1-6. 2. Zou K, et al. J Biol Chem, 2009, 284(46), 31914-31920. 3. Yasumatsu R, et al. J Cancer Res Clin Oncol, 2004, 130(10), 567-573. 4. Yoshiji H, et al. Clin Cancer Res, 2001, 7(4), 1073-1078. 5. Ceconi C, et al. Cardiovasc Drugs Ther, 2007, 21(6), 423-429.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Membrane Protein-targeted Compound Library Inhibitor Library Drug Repurposing Compound Library Nonsteroidal Anti-Inflammatory Compound Library ReFRAME Related Library Bioactive Compound Library Clinical Compound Library

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Keywords

Perindopril erbumine 107133-36-8 Apoptosis Endocrinology/Hormones Immunology/Inflammation MRP RAAS S 9490 inhibit Perindopril S-9490 Inhibitor S9490-3 Perindopril tert-butylamine Angiotensin-converting Enzyme (ACE) S9490 Perindopril tert-butylamine salt inhibitor

 

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