Perindopril erbumine

SKU: orb1308507

Description

Perindopril erbumine is the prodrug form of perindoprilat, an angiotensin-converting enzyme (ACE) inhibitor. Upon activation, it blocks the formation of angiotensin II, leading to vasodilation and reduced aldosterone secretion. This compound is widely used in cardiovascular research, including in vitro enzyme assays and in vivo models of hypertension.

Research Area

Cell Biology, Epigenetics & Chromatin, Immunology & Inflammation, Metabolism Research, Molecular Biology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 107133-36-8
• MW: 441.61
• Purity: 99.94%
• Formula: C₂₃H₄₃N₃O₅
• 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
• Target: Angiotensin-converting Enzyme (ACE),Sirtuin,MRP,STAT,NF-κB,Apoptosis,RAAS
• Solubility: DMSO:50 mg/mL (113.22 mM);H2O:50 mg/mL (113.22 mM)

Bioactivity

• Target IC50:
  ACE:1.05 nM
• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, MRP1, Inhibitor, Apoptosis, Angiotensin-converting Enzyme (ACE), ACE, S9490, S-9490, S9490-3, S 9490, Perindopril erbumine, Perindopril tert-butylamine, Perindopril tert-butylamine salt, Perindopril

Compound Identifiers

PubChem CID

441313