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Enalapril Maleate

Enalapril Maleate

产品编号 T6486   CAS 76095-16-4
别名: MK-421 Maleate, Renitec Maleate, Glioten Maleate, MK-421 (maleate), Vasotec Maleate, 马来酸依那普利

Enalapril Maleate (MK-421 Maleate) 一种是血管紧张素转化酶(ACE)抑制剂。

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Enalapril Maleate Chemical Structure
Enalapril Maleate, CAS 76095-16-4
规格 价格/CNY 货期 数量
500 mg ¥ 147 现货
其他形式的 Enalapril Maleate:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
产品目录号及名称: Enalapril Maleate (T6486)
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纯度: 99.54%
纯度: 99.02%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 4 mg/mL (8.12 mM)

DMSO: 92 mg/mL (186.8 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

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

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TargetMol Library Books参考文献

1. Vlasses PH, et al. Clin Pharm,1985, 4(1), 27-40. 2. Knowles JW, et al. J Clin Invest,2000, 105(4), 451-458. 3. Cozzoli A, et al. Pharmacol Res,2011, 64(5), 482-492. 4. Itoh Y, et al. J Endocrinol,2002, 175(1), 233-239.
OPHIOPOGONIN D ANGIOTENSIN IV TFA(12676-15-2(free base)) Benazepril hydrochloride Captopril Leucylarginylproline Losartan Carboxylic Acid Prosaikogenin G Angiotensin 1/2 (5-7) acetate

相关化合物库

该产品包含在如下化合物库中:
膜蛋白靶向化合物库 EMA 上市药物库 抑制剂库 药物功能重定位化合物库 上市药物库 表型筛选靶点鉴定库 抗代谢疾病化合物库 FDA 上市药物库 已知活性化合物库 儿童药物库

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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。

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Keywords

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

 

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