MLN-4760

For research use only. Not for use in humans.

目录号:S8940

MLN-4760 Chemical Structure

CAS No. 305335-31-3

MLN-4760 (compound 16) 是一种有效的、选择性的人 angiotensin-converting enzyme 2 (ACE2) 的抑制剂,IC50值为0.44 nM。MLN-4760 还抑制 bovine carboxypeptidase A (CPDA),其IC50值为27 μM。

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产品安全说明书

ACE抑制剂选择性比较

生物活性

产品描述 MLN-4760 (compound 16) 是一种有效的、选择性的人 angiotensin-converting enzyme 2 (ACE2) 的抑制剂,IC50值为0.44 nM。MLN-4760 还抑制 bovine carboxypeptidase A (CPDA),其IC50值为27 μM。
靶点
ACE2 [1]
(Cell-free assay)
CPDA [1]
(Cell-free assay)
0.44 nM 27 μM
体外研究

In vitro, conversion from angiotensin II to angiotensin-(1–7) by mouse ACE2 is blocked by MLN-4760 (10 μM). MLN-4760 inhibits both human and mouse ACE2 activity.[3] In huMNCs, MLN-4760-B (an isomer of MLN-4760) detects 63% ACE2 with 28-fold selectivity over ACE. In huCD34+ cells, MLN-4760-B detects 38% of ACE2 activity with 63-fold selectivity. In mu-heart and muMNCs, MLN-4760-B is 100- and 228-fold selective for ACE2, respectively. In muLin- cells, MLN-4760-B detects 25% ACE2 activity with a pIC50 of 6.3. The racemic mixture and MLN-4760-A shows lower efficacy and poor selectivity for ACE2 in MNCs and mu-heart.[4]

体内研究

MLN-4760 blocks ACE2 activity, thus significantly reverses the elevation of carotid Ang-(1-7) level and the decline of carotid Ang II level induced by NaHS in mice. The anti-atherosclerotic property of NaHS is also significantly abolished by treatment with MLN-4760.[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:

[4]

- 合并
  • Cell lines: mononuclear cells (MNCs), huCD34+ cells, mu-lineage-depleted (muLin-) cells
  • Concentrations: 0.01 nM to 300 μM
  • Incubation Time: 1 h, 4 h
  • Method:

    In the case of cell lysates, 10 μg of total protein is assayed for activity in a buffer with the following composition: 50mM MES (4-morpholineethanesulphonic acid), 300mM NaCl, 10μM ZnCl2 and 0.01% Triton X-100, pH 6.5. Reaction is initiated by the addition of 5×10-5 M substrate. Where applicable, recombinant enzymes are used at a concentration of 0.01 μg per reaction. The fluorescence measurements are performed in the black microtiter plates in a total volume of 100 μl. The plates are read using a fluorescence plate reader SpectraMax M5 at an excitation wavelength 320 nm and emission wavelength 405 nm Fluorescence resulting from the substrate hydrolysis increased with time, and achieved maximum by 1 h with recombinant enzyme however with cell/tissue lysates the maximum fluorescence is observed by 4 h of incubation. Therefore fluorescence recorded at 1 and 4 h of reaction time is taken for calculation of percent enzyme inhibition, when using recombinant enzymes and cell/tissue lysates, respectively. ACE2 activity is defined as the ACE2 inhibitor-sensitive fluorescence and ACE activity is defined as the ACE inhibitor, captopril-sensitive fluorescence, and are expressed as percent inhibition. Unless specified, MLN4760 is used in concentration ranging from 0.01 nM to 300 μM.


    (Only for Reference)
动物实验:

[2]

- 合并
  • Animal Models: C57BL/6J male apoE−/− mice
  • Dosages: 0.5 mg/kg
  • Administration: IP
    (Only for Reference)

溶解度 (25°C)

体外 Water 86 mg/mL (200.78 mM)
DMSO Insoluble
Ethanol '''10 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 428.31
化学式
C19H23Cl2N3O4
CAS号 305335-31-3
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID