5.30616
MLN-4760
≥97% (HPLC), Angiotensin-converting enzyme 2 inhibitor, powder
别名:
ACE2抑制剂，MLN-4760
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关于此项目
经验公式（希尔记法）:
C19H23Cl2N3O4
化学文摘社编号:
分子量:
428.31
MDL number:
UNSPSC Code:
51111800
NACRES:
NA.77
产品名称
ACE2抑制剂，MLN-4760, ≥97% (HPLC), powder, Calbiochem®
SMILES string
Clc1cc(cc(c1)C[n]2cncc2C[C@H](N[C@@H](CC(C)C)C(=O)O)C(=O)O)Cl
InChI
1S/C19H23Cl2N3O4/c1-11(2)3-16(18(25)26)23-17(19(27)28)7-15-8-22-10-24(15)9-12-4-13(20)6-14(21)5-12/h4-6,8,10-11,16-17,23H,3,7,9H2,1-2H3,(H,25,26)(H,27,28)/t16-,17-/m0/s1
InChI key
NTCCRGGIJNDEAB-IRXDYDNUSA-N
assay
≥97% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
technique(s)
inhibition assay: suitable
color
white
solubility
DMSO: 100 mg/mL
storage temp.
2-8°C
Quality Level
相关类别
General description
MLN-4760是血管紧张素转换酶2的高效和选择性细胞渗透性抑制剂，这是其主要靶标。（ACE2；可溶性人ACE2的IC50=440 pM）。
Biochem/physiol Actions
MLN-4760 具有生物可利用性，并且对羧肽酶（50 pM人ACE2的IC50=0.44 nM；[ZnCl2]=10 μM， [MCA-APK（DNP）]=50 μM）的选择性远高于牛羧肽酶 A 或 ACE 肽基二肽酶活性（0.5 nM牛CPDA和1 nM猪ACE的IC50分别为=27 μM和>100 μM；[底物]=50 μM）和猪 ACE（分别为IC50=27和>100 μM）这种可逆的ACE2抑制剂以高亲和力与活性位点锌结合，并模拟肽水解过程中的过渡态。其降低了小鼠的血清和肾脏ACE 2活性，并消除血管紧张素II诱导的高血压。MLN-4760选择性地阻断在低ANG II浓度（<0.1 μM）下ACE2野生型（WT）小鼠中血管紧张素（ANG-（1-7））的形成，但在较高ANG II浓度下它不影响小鼠中的ANG-（1-7）水平。这种ACE2抑制剂在体外增强了鼠内皮细胞中肿瘤坏死因子（TNF）（10 pg/ml）刺激的促炎细胞因子的表达（使用SVEC-40系和原代主动脉内皮培养物为1 μM）。MLN-4760被广泛用于研究ACE2在肾脏，心血管和炎症性肠病中的作用，通过饮用水（10 mg/kg/d），静脉注射（0.1 mg/kg），和皮下注射（30 mg/kg/d至300 mg/kg/12 h）在大鼠和小鼠体内。已显示抑制剂亮氨酸部分通过其羧酸盐同时靶向具有异丁基和活性位点锌的ACE2底物S1口袋，而化合物′3，5-二氯苄基有效地占据了S1′亚位。
MLN-4760还能够研究降低的ACE2活性对肺部对冠状病毒病（COVID）相关急性呼吸窘迫综合征（ARDS）的易感性的影响。
MLN-4760还能够研究降低的ACE2活性对肺部对冠状病毒病（COVID）相关急性呼吸窘迫综合征（ARDS）的易感性的影响。
Packaging
用惰性气体包装
Preparation Note
复溶后，等分并冷冻保存（-20°C）。贮备液在-20°C下可稳定保存至多6个月。
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
毒性：标准处理（A）
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Minghao Ye et al.
Hypertension (Dallas, Tex. : 1979), 60(3), 730-740 (2012-07-11)
A newly produced murine recombinant angiotensin (Ang)-converting enzyme 2 (ACE2) was characterized in vivo and in vitro. The effects of available ACE2 inhibitors (MLN-4760 and 2 conformational variants of DX600, linear and cyclic) were also examined. When murine ACE2 was
Aaron J Trask et al.
American journal of hypertension, 23(6), 687-693 (2010-03-20)
Emerging evidence suggests that cardiac angiotensin-converting enzyme 2 (ACE2) may contribute to the regulation of heart function and hypertension-induced cardiac remodeling. We tested the hypothesis that inhibition of ACE2 in the hearts of (mRen2)27 hypertensive rats may accelerate progression of
Paul Towler et al.
The Journal of biological chemistry, 279(17), 17996-18007 (2004-02-03)
The angiotensin-converting enzyme (ACE)-related carboxypeptidase, ACE2, is a type I integral membrane protein of 805 amino acids that contains one HEXXH + E zinc-binding consensus sequence. ACE2 has been implicated in the regulation of heart function and also as a
M J Soler et al.
Kidney international, 72(5), 614-623 (2007-06-21)
Angiotensin converting enzyme 2 (ACE2) is localized to the glomerular epithelial cells. Since ACE2 promotes the degradation of angiotensin II, a decrease in ACE2 activity could lead to the development of glomerular injury. We gave a specific ACE2 inhibitor, MLN-4760
John J Byrnes et al.
Inflammation research : official journal of the European Histamine Research Society ... [et al.], 58(11), 819-827 (2009-06-12)
Angiotensin-converting enzyme 2 (ACE2) is expressed in gastrointestinal tissue. Previous studies of GL1001, a potent and selective ACE2 inhibitor, have revealed anti-inflammatory activity in the mouse digestive tract. We hypothesized that GL1001 might also produce beneficial effects in a mouse
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