Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Enalapril Maleate (MK-421 Maleate) 一种是血管紧张素转化酶(ACE)抑制剂。
产品描述 | Enalapril Maleate (MK-421 Maleate), an angiotensin-converting enzyme (ACE) inhibitor, is utilized in the treatment of hypertension, chronic heart failure , and diabetic nephropathy. |
体外活性 | Enalapril?is rapidly converted by ester hydrolysis to enalaprilat, a potent ACE?inhibitor;?Enalapril?itself is only a weak ACE?inhibitor.?Enalapril?lowers peripheral vascular resistance without causing an increase in heart rate.?[1] |
体内活性 | Enalapril?treatment?abolishes the deleterious effects of?eNOS?deficiency on blood pressure (BP),?atherosclerosis, and?kidney dysfunction?in nnee?mice. [2] Enalapril?causes a dose-dependent increase in fore limb strength?in the?mdx?mouse. Enalapril?causes a dose-dependent reduction of superoxide anion production?in tibialis anterior?muscle?of the?mdx?mouse as observed by dihydroethidium staining.?Enalapril?(5 mg/kg) reduces the area of?muscle?necrosis in both gastrocnemious?muscle?and diaphragm, without significant effect on non-muscle?area. [3] Enalapril Maleate results in significant increases in kidney weight and in concentrations of urinary albumin, N-acetyl-fl-d-glucosamidase (NAG) and serum ET-1 in streptozotocin (STZ)-induced?diabetic (STZ-DM)?rats as compared with the non-diabetic?rats, and the concentration of ET-1 in the kidneys tended to be increased. Enalapril Maleate results in increased mesangial cell proliferation, matrix expansion and enlarged mesangial area in the kidney of the?diabetic?rats.?Enalapril Maleate reduces increased concentrations of urinary albumin and NAG in the STZ-DM?rats to the control values with a slight improvement in the electron microscopic?changes.[4] |
激酶实验 | Single displacement binding assay: The binding assay is based on the competitive displacement of [125I]351A by Enalaprilat performed on whole endothelial cells. Subconfluent HUVECs in 6-well plates are rinsed with 2 mL binding buffer (140 mM NaCl, 2.7 mM KCl, 1.8 mM CaCl2, 1.03 mM MgCl2, 0.42 mM NaH2PO4, 10 mM HEPES, 2 mM sodium pyruvate and 5 mM glucose, pH 7.4), and the culture medium is replaced with 2.5 mL fresh binding buffer containing 5% fetal bovine serum (FBS). The Enalaprilat (2.5-12.5 μL, 0.1-50 nM) or equivalent volumes of diluent are added to the binding buffer. A saturating amount of [125I]351A (10 μL, typically 106 cpm) is then added to each sample and the plates are incubated at 37 °C for 2 hours in a thermostatic bath. The cells are then rinsed twice with 1.5 mL binding buffer. Finally, the cells are extracted with 0.5 mL NaOH 1 N, incubated for 5 minutes, and the radioactivity is counted with a gamma counter. The ratio of specific [125I]351A bound to total bound activity (B/B0) is calculated, and the inhibitory potency of Enalaprilat expressed as the concentration of ACE inhibitors able to displace 50% of the bound radioligand, i.e. the IC50. |
别名 | MK-421 Maleate, Renitec Maleate, Glioten Maleate, MK-421 (maleate), Vasotec Maleate, 马来酸依那普利 |
分子量 | 492.52 |
分子式 | C20H28N2O5·C4H4O4 |
CAS No. | 76095-16-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 4 mg/mL (8.12 mM)
DMSO: 92 mg/mL (186.8 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.0304 mL | 10.1519 mL | 20.3037 mL | 50.7594 mL |
5 mM | 0.4061 mL | 2.0304 mL | 4.0607 mL | 10.1519 mL | |
DMSO | 10 mM | 0.203 mL | 1.0152 mL | 2.0304 mL | 5.0759 mL |
20 mM | 0.1015 mL | 0.5076 mL | 1.0152 mL | 2.538 mL | |
50 mM | 0.0406 mL | 0.203 mL | 0.4061 mL | 1.0152 mL | |
100 mM | 0.0203 mL | 0.1015 mL | 0.203 mL | 0.5076 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Enalapril Maleate 76095-16-4 Endocrinology/Hormones RAAS Enalapril inhibit Angiotensin-converting Enzyme (ACE) Inhibitor MK 421 Maleate MK-421 Maleate Renitec Maleate Glioten Maleate MK-421 MK-421 (maleate) MK 421 MK421 MK421 Maleate Vasotec Maleate 马来酸依那普利 inhibitor