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质量水平
检测方案
≥97% (HPLC)
形式
powder
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
技术
inhibition assay: suitable
颜色
white
溶解性
DMSO: 100 mg/mL
储存温度
2-8°C
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
一般描述
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）。
生化/生理作用
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。
包装
用惰性气体包装
警告
毒性：标准处理（A）
重悬
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。
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 1
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Shrinidh Joshi et al.
European journal of pharmacology, 774, 25-33 (2016-02-07)
Angiotensin-converting enzymes, ACE and ACE2, are key members of renin angiotensin system. Activation of ACE2/Ang-(1-7) pathway enhances cardiovascular protective functions of bone marrow-derived stem/progenitor cells. The current study evaluated the selectivity of ACE2 inhibitors, MLN-4760 and DX-600, and ACE and
Merlin C Thomas et al.
Circulation research, 107(7), 888-897 (2010-07-31)
Angiotensin-converting enzyme (ACE)2 opposes the actions of angiotensin (Ang) II by degrading it to Ang 1-7. Given the important role of Ang II/Ang 1-7 in atherogenesis, we investigated the impact of ACE2 deficiency on the development of atherosclerosis. C57Bl6, Ace2
Nadja Grobe et al.
American journal of physiology. Cell physiology, 304(10), C945-C953 (2013-02-09)
Angiotensin-converting enzyme 2 (ACE2) catalyzes conversion of ANG II to ANG-(1-7). The present study uses newly established proteomic approaches and genetic mouse models to examine the contribution of alternative renal peptidases to ACE2-independent formation of ANG-(1-7). In situ and in
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
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