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Enalaprilat Dihydrate

产品编号 T6340 CAS 84680-54-6

别名: 依那普利拉二水合物, MK-422, MK-422 Dihydrate

Enalaprilat Dihydrate (MK-422 Dihydrate) 是一种有效的血管紧张素转化酶抑制剂，IC50为 1.94 nM。

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Enalaprilat Dihydrate Chemical Structure

Enalaprilat Dihydrate, CAS 84680-54-6

规格	价格/CNY	货期
25 mg	￥ 343	现货
50 mg	￥ 497	现货
100 mg	￥ 872	现货
200 mg	￥ 1,480	待询
1 mL * 10 mM (in DMSO)	￥ 739	现货

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其他形式的 Enalaprilat Dihydrate:

选择批次

纯度: 99.78%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Enalaprilat Dihydrate (MK-422 Dihydrate) （IC50=1.94 nM） is a potent angiotensin-converting enzyme (ACE) inhibitor.
靶点活性	ACE:1.94 nM
体外活性	Enalaprilat has high affinity for human endothelial ACE with IC50 of 1.94 nM in vitro binding assay by displacing a saturating concentration of [125I]351A, a radiolabeled lisinopril analogue from ACE binding sites, and shows bradykinin/angiotensin I selectivity ratio of 1.00 calculated from double displacement experiments. [1] Enalaprilat has the strong inhibitory effect on Aβ42-to-Aβ40-converting activity found in the N-domain of ACE, exhibiting a 10-fold lower IC50 (0.003~0.01 μM) than captopril (0.03~0.1 μM). [2] Enalaprilat (100 nM) blocks protein kinase C epsilon by directly activating bradykinin B1 receptor at the canonical Zn2+ binding site, leading to prolonged nitric oxide (NO) production in cytokine-treated human lung microvascular endothelial cells. [3] Enalaprilat attenuates the IGF-I induced neonatal rat cardiac fibroblast growth (30% reduction) in a concentration-dependent fashion, with IC50 of 90 mM. [4]
体内活性	Enalaprilat has unfavourable ionisation characteristics to allow sufficient potency for oral administration, thus Enalaprilat is only suitable for intravenous administration, which is overcome by the esterification with ethanol to produce Enalapril. Administration of Enalaprilat induces a significant reduction of MAP at 70 minutes compared with the placebo group during haemorrhagic shock in rats, and results in a 50% reduction of CO, a general tendency of EB extravasation which is significant in the kidney and lungs, and a significant increase in ileal EB extravasation (53%). [5] Enalaprilat has no effect in nonhypertrophied hearts, but significantly attenuates the greater increase in left ventricular end-diastolic pressure in hypertrophied hearts compared with no drug. [6]
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.
细胞实验	After 24 hours incubation in serum-free medium (DMEM), cells are stimulated with IGF-I (1-100 nM) and coincubated with Enalaprilat (1 nM-10 μM) for 24 hours. Cellular proliferation is assessed by 5-bromo-2'-deoxyuridine (BrdU) incorporation during the last 4 hours of the 24 hours incubation period using a colorimetric immunoassay. The extinctions are measured at 450 nm in an ELISA plate reader. All values consist of an n=9.(Only for Reference)

别名	依那普利拉二水合物, MK-422, MK-422 Dihydrate
分子量	348.4
分子式	C18H24N2O5·2H2O
CAS No.	84680-54-6

存储

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

溶解度

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

DMSO: 70 mg/mL (200.91 mM)

Ethanol: < 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
DMSO	1 mM	2.8703 mL	14.3513 mL	28.7026 mL	71.7566 mL
	5 mM	0.5741 mL	2.8703 mL	5.7405 mL	14.3513 mL
	10 mM	0.287 mL	1.4351 mL	2.8703 mL	7.1757 mL
	20 mM	0.1435 mL	0.7176 mL	1.4351 mL	3.5878 mL
	50 mM	0.0574 mL	0.287 mL	0.5741 mL	1.4351 mL
	100 mM	0.0287 mL	0.1435 mL	0.287 mL	0.7176 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Ceconi C, et al. Eur J Pharmacol, 2007, 577(1-3), 1-6. 2. Zou K, et al. J Biol Chem, 2009, 284(46), 31914-31920. 3. Stanisavljevic S, et al. J Pharmacol Exp Ther, 2006, 316(3), 1153-1158. 4. van Eickels M, et al. Br J Pharmacol, 2000, 131(8), 1592-1596. 5. Schumacher J, et al. Br J Anaesth, 2006, 96(4), 437-443.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

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。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

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。

Keywords

Enalaprilat Dihydrate 84680-54-6 Autophagy Endocrinology/Hormones RAAS Inhibitor hypertension inhibit MK 422 Dihydrate angiotensin I angiotensin II 依那普利拉二水合物 Angiotensin-converting Enzyme (ACE) MK 422 MK-422 MK422 Dihydrate MK422 Enalaprilat MK-422 Dihydrate inhibitor

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Enalaprilat Dihydrate

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords