Perindopril erbumine NEW
Price | $30 | $41 | $63 |
Package | 50mg | 100mg | 200mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-15 |
Product Details
Product Name: Perindopril erbumine | CAS No.: 107133-36-8 |
Purity: 99.75% | Supply Ability: 10g |
Release date: 2024/11/15 |
Product Introduction
Bioactivity
名稱 | Perindopril erbumine |
描述 | 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. |
體外活性 | 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. |
體內(nèi)活性 | 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. |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | H2O : 50 mg/mL (113.22 mM) DMSO : 50 mg/mL (113.22 mM), Sonication is recommended. |
關(guān)鍵字 | S 9490 | inhibit | Perindopril | S-9490 | Inhibitor | Perindopril tert-butylamine | Angiotensin-converting Enzyme (ACE) | S9490 | Perindopril erbumine | Apoptosis |
相關(guān)產(chǎn)品 | Stavudine | 5-Fluorouracil | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Captopril |
相關(guān)庫 | 經(jīng)典已知活性庫 | 膜蛋白靶向化合物庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | NO PAINS 化合物庫 | FDA 上市藥物庫 | 抗癌上市藥物庫 | 已知活性化合物庫 | 抗癌藥物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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