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Perindopril Erbumine/培哚普利叔丁胺 {[allProObj[0].p_purity_real_show]}

货号:A628131 同义名: 培哚普利叔丁胺 / Perindopril tert-butylamine salt; S-9490 erbumine

Perindopril Erbumine 是一种长效 ACE 抑制剂(IC50 = 1.05 nM),常用于高血压的研究。

Perindopril Erbumine/培哚普利叔丁胺 化学结构 CAS号:107133-36-8
Perindopril Erbumine/培哚普利叔丁胺 化学结构
CAS号:107133-36-8
Perindopril Erbumine/培哚普利叔丁胺 3D分子结构
CAS号:107133-36-8
Perindopril Erbumine/培哚普利叔丁胺 化学结构 CAS号:107133-36-8
Perindopril Erbumine/培哚普利叔丁胺 3D分子结构 CAS号:107133-36-8
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Perindopril Erbumine/培哚普利叔丁胺 生物活性

靶点
  • ACE

    ACE, IC50:1.05 nM

描述 Perindopril erbumine is a potent ACE inhibitor of which is used to treat high blood pressure, heart failure or stable coronary artery disease. Target: ACE Perindopril is a long-acting ACE inhibitor[3]. It is indicated for the treatment of essential hypertension either alone or in combination with other antihypertensives, especially thiazide diuretics[4]. Perindopril is effective and safe for blood pressure control with a dose-dependent effect. Perindopril in combination with amlodipine significantly reduced total and cardiovascular mortality as compared to atenolol/diuretic in large-scale clinical trials of hypertensive patients[5]. Perindopril 4 to 8 mg once daily significantly reduces supine systolic blood pressure (SBP) and diastolic blood pressure (DBP) from baseline values in hypertensive patients. Perindopril 4 to 8 mg once daily significantly decreased carotid-femoral aortic pulse wave velocity (PWV), improved arterial compliance, reduced left ventricular mass index and, in patients with recent cerebral ischaemia and/or stroke, preserved cerebral blood flow despite significantly reducing SBP and DBP[6].

Perindopril Erbumine/培哚普利叔丁胺 细胞实验

Cell Line
Concentration Treated Time Description References
Chang cells 0.156, 0.313, 0.625, 1.25, 2.5, 5.0, 10.0 µg/mL 24 hours To evaluate cytotoxicity, results showed that perindopril, PMAE, and Mg/Al-layered double hydroxide had no toxic effects on Chang cells at concentrations up to 10.0 µg/mL. Int J Nanomedicine. 2012;7:4251-62

Perindopril Erbumine/培哚普利叔丁胺 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Wistar rats Aluminum chloride (AlCl3) induced Alzheimer's disease model Oral 0.5 mg/kg/day and 1 mg/kg/day Once daily for consecutive 60 days To evaluate the protective effect of perindopril and azilsartan as monotherapy or in combination on aluminum chloride (AlCl3) induced neurobehavioral and pathological changes. Results showed that oral administration of either azilsartan and perindopril alone or in combined for 60 days have shown improvement of cognitive function, significant reduction in the hippocampal levels of Aβ-42, Acetylcholinesterase, Malondialdehyde (MDA), Tumor necrosis factor (TNF-α) and reserved most of histopathological changes in dentate gyrus (DG) and Cornu Ammonis-3 (CA3) that mediated by Alcl3. Saudi Pharm J. 2020 May;28(5):574-581
New Zealand rabbits Ischemic heart failure model Oral 0.66 mg/kg/day Once daily for 4 weeks To evaluate the effects of perindopril on ventricular remodeling and myocardial fibrosis in rabbits with ischemic heart failure. Results showed that perindopril significantly improved cardiac function and reduced myocardial fibrosis. Front Physiol. 2019 Mar 22;10:267
Balb/c male mice DSS-induced colitis model Oral gavage 1 mg/kg/day Once daily for one week Perindopril alone or in combination with ambrosin ameliorated DSS-induced colitis in mice by modulating TLR4/NF-κB signaling and SIRT1/PPAR-γ levels, reducing oxidative stress and inflammatory responses, and improving histopathological and electron microscopic changes in colonic tissues. Pharmaceuticals (Basel). 2022 May 13;15(5):600
Mice DENA-induced hepatocellular carcinoma model Oral 1 mg/kg/day Once daily for four weeks Perindopril, whether used alone or in combination with sorafenib, decreased liver enzymes and preserved liver architecture. The study revealed that perindopril significantly enhanced the antineoplastic, antiangiogenic, and anti-metastatic effects of sorafenib. This effect was associated with the downregulation of the leptin/Wnt/β-catenin pathway, overexpression of ALDH1, and downregulation of EpCAM. Saudi Pharm J. 2022 Aug;30(8):1170-1180

Perindopril Erbumine/培哚普利叔丁胺 参考文献

[1]Zou K, Maeda T, et al. Abeta42-to-Abeta40- and angiotensin-converting activities in different domains of angiotensin-converting enzyme. J Biol Chem. 2009 Nov 13;284(46):31914-20.

[2]Ceconi C, Francolini G, et al. Angiotensin-converting enzyme (ACE) inhibitors have different selectivity for bradykinin binding sites of human somatic ACE. Eur J Pharmacol. 2007 Dec 22;577(1-3):1-6.

[3]áclavík J. Perindopril v léčbě hypertenze a kardiovaskulárních chorob: evoluce pokračuje orodisperzní formou [Perindopril in the treatment of hypertension and cardiovascular diseases: evolution continues with the orodispersible dosage form]. Vnitr Lek. 2013 Apr;59(4):290-4. Czech

[4]O'Loughlin DC, Chu VL, Singh D. Perindopril. Heart Dis. 2000 Nov-Dec;2(6):446-55

[5]Ghiadoni L. Perindopril for the treatment of hypertension. Expert Opin Pharmacother. 2011 Jul;12(10):1633-42

[6]Hurst M, Jarvis B. Perindopril: an updated review of its use in hypertension. Drugs. 2001;61(6):867-96

Perindopril Erbumine/培哚普利叔丁胺 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.26mL

0.45mL

0.23mL

11.32mL

2.26mL

1.13mL

22.64mL

4.53mL

2.26mL

Perindopril Erbumine/培哚普利叔丁胺 技术信息

CAS号107133-36-8
分子式C23H43N3O5
分子量 441.6
SMILES Code O=C([C@H]1N(C([C@@H](N[C@H](C(OCC)=O)CCC)C)=O)[C@@]2([H])CCCC[C@@]2([H])C1)O.CC(C)(C)N
MDL No. MFCD02313824
别名 培哚普利叔丁胺 ;Perindopril tert-butylamine salt; S-9490 erbumine; S9490-3
运输蓝冰
InChI Key IYNMDWMQHSMDDE-MHXJNQAMSA-N
Pubchem ID 441313
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, room temperature

溶解方案

DMSO: 9 mg/mL(20.38 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 50 mg/mL(113.22 mM)

配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
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