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Perindopril Erbumine

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Chemical Structure| 107133-36-8 同义名 : 培哚普利叔丁胺 ;Perindopril tert-butylamine salt;S-9490 erbumine;S9490-3
CAS号 : 107133-36-8
货号 : A628131
分子式 : C23H43N3O5
纯度 : 99%
分子量 : 441.6
MDL号 : MFCD02313824
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

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)
动物实验配方：
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].
实验方案
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
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