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Lisinopril/赖诺普利 {[allProObj[0].p_purity_real_show]}

货号：A285815 同义名： MK-521; MK-522

Lisinopril is angiotensin-converting enzyme inhibitor that blocks the formation of angiotensin I with an IC50 value of 1.2 nM (ovine) and displays ID50 values of 2.3 and 6.5 µg/kg in rat and canine, respectively. It is used in treatment of hypertension, congestive heart failure, and heart attacks.

Lisinopril/赖诺普利 化学结构 CAS号：76547-98-3
Lisinopril/赖诺普利 化学结构
CAS号：76547-98-3
Lisinopril/赖诺普利 3D分子结构
CAS号：76547-98-3
Lisinopril/赖诺普利 化学结构 CAS号：76547-98-3
Lisinopril/赖诺普利 3D分子结构 CAS号：76547-98-3
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Lisinopril/赖诺普利 纯度/质量文件 产品仅供科研

货号：A285815 标准纯度： {[allProObj[0].p_purity_real_show]}
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Lisinopril/赖诺普利 生物活性

描述 Angiotensin-converting enzyme (ACE) is responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII), which regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS) [3]. Lisinopril (MK-521) is angiotensin-converting enzyme inhibitor with inhibition constant (Ki) value of 0.39 mM, used in treatment of hypertension, congestive heart failure, and heart attacks[4]. Although lisinopril significantly reduced preload, its effect on left ventricular (LV) contractility was insignificant in experimental mitral regurgitation (MR). Conversely, atenolol, when added to lisinopril, achieved maximum hemodynamic benefit and also restored LV contractility [5]. In spontaneously hypertensive rats (SHR) rats, levels of α-tocopherol were substantially reduced in both plasma and cardiac tissue. Treatment with lisinopril ameliorated reduced levels of plasma α-tocopherol in SHR rats [6]. Paraquat caused a significant increase in hydroxyproline content and lisinopril significantly decreased the amount hydroxyproline (p<0.001) in the lung tissue of the rats. The histological examination also indicated that lisinopril can effectively protect the paraquat-induced lung fibrosis [7]. In isolated guinea pig hearts, lisinopril protects the cell membrane integrity and lessens free radical-induced oxidant stress [8].

Lisinopril/赖诺普利 动物研究

Dose Rat: 0.225 mg/kg, 0.45 mg/kg[3] (p.o.)， 4 mg/kg - 20 mg/kg[4] (p.o.), 50 mg/kg[5] (p.o.); 2 mg/kg - 50 mg/kg[6] (s.c.)
Administration p.o., s.c.

Lisinopril/赖诺普利 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00567307 Cardiovascular Disease Phase 2 Completed - Sri Lanka ... 展开 >> The National Hospital of Sri Lanka Colombo, Sri Lanka, Colombo10 Teaching (General) Hospital Kandy Kandy, Sri Lanka Teaching (General) Hospital Kegalle Kegalle, Sri Lanka 收起 <<
NCT00292162 Chronic Heart Failure ... 展开 >> Atrial Fibrillation 收起 << Not Applicable Completed - United Kingdom ... 展开 >> Glasgow Royal Infirmary Glasgow, Scotland, United Kingdom, G31 2ER 收起 <<
NCT03461003 Pediatric Hypertension Phase 4 Recruiting January 2020 United States, Texas ... 展开 >> The University of Texas Health Science Center at Houston Recruiting Houston, Texas, United States, 77030 Contact: Joyce P Samuel, MD, MS    713-500-5670    joyce.p.samuel@uth.tmc.edu 收起 <<

Lisinopril/赖诺普利 参考文献

[1]Andujar-Sanchez, M., V. Jara-Perez, and A. Camara-Artigas, Thermodynamic determination of the binding constants of angiotensin-converting enzyme inhibitors by a displacement method. FEBS Lett, 2007. 581(18): p. 3449-54.

[2]Gomez HJ, Cirillo VJ, Moncloa F. The clinical pharmacology of lisinopril. J Cardiovasc Pharmacol. 1987;9 Suppl 3:S27-34.

[3]Song JC. Clinical pharmacokinetics and selective pharmacodynamics of new angiotensin converting enzyme inhibitors: an update. Clin Pharmacokinet. 2002;41(3):207-24. doi: 10.2165/00003088-200241030-00005.

[4]Swaan PW. Molecular mechanism for the relative binding affinity to the intestinal peptide carrier. Comparison of three ACE-inhibitors: enalapril, enalaprilat, and lisinopril. Biochim Biophys Acta. 1995 May 24;1236(1):31-8. doi: 10.1016/0005-2736(95)00030-7.

[5]Nemoto S. Differential effects of the angiotensin-converting enzyme inhibitor lisinopril versus the beta-adrenergic receptor blocker atenolol on hemodynamics and left ventricular contractile function in experimental mitral regurgitation. J Am Coll Cardiol. 2002 Jul 3;40(1):149-54. doi: 10.1016/s0735-1097(02)01926-5.

[6]Mantle D. Effects of lisinopril and amlodipine on antioxidant status in experimental hypertension. Clin Chim Acta. 2000 Sep;299(1-2):1-10. doi: 10.1016/s0009-8981(00)00270-9.

[7]Mohammadi-Karakani A, Ghazi-Khansari M, Sotoudeh M. Lisinopril ameliorates paraquat-induced lung fibrosis. Clin Chim Acta. 2006 May;367(1-2):170-4. doi: 10.1016/j.cca.2005.12.012. Epub 2006 Feb 3.

[8]Selim Isbir C. The protective effect of lisinopril on membrane-bound enzymes in myocardial preservation. Cell Biochem Funct. 2000 Jun;18(2):85-91.

Lisinopril/赖诺普利 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.47mL

0.49mL

0.25mL

12.33mL

2.47mL

1.23mL

24.66mL

4.93mL

2.47mL

Lisinopril/赖诺普利 技术信息

CAS号76547-98-3
分子式C21H31N3O5
分子量 405.49
SMILES Code O=C([C@H]1N(CCC1)C([C@@H](N[C@@H](CCC2=CC=CC=C2)C(O)=O)CCCCN)=O)O
MDL No. MFCD00214086
别名 MK-521; MK-522
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

Tags: Lisinopril | 76547-98-3 | MK-521 | MK521 | MK 521 | ACE Inhibitor | Metabolic Enzyme/Protease | Angiotensin-converting Enzyme (ACE) | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Lisinopril/赖诺普利 纯度/质量文件 | Lisinopril/赖诺普利 生物活性 | Lisinopril/赖诺普利 动物研究 | Lisinopril/赖诺普利 临床数据 | Lisinopril/赖诺普利 参考文献 | Lisinopril/赖诺普利 实验方案 | Lisinopril/赖诺普利 技术信息

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