MLN-4760 （ACE2抑制剂）-上海雅吉生物科技有限公司

规格	价格	库存
10mM×0.2ml	￥ 899	200
5mg	￥ 2899	200
25mg	￥ 7999	200
100mg	￥ 26000	200

化学名	2( S)-(1( S)-Carboxy-2-(3-(3,5-dichlorobenzyl)-3H-imidazol-4-yl)-ethylamino)-4-methylpentanoic acid
简称	MLN-4760, ACE2 Inhibitor
别名	Angiotensin-Converting Enzyme-Related Carboxypeptidase Inhibitor, ML00106791, GL-1001, GL1001, MLN4760
中文名	-
化学式	C19H23Cl2N3O4
分子量	428.31
CAS号	305335-31-3
纯度	>96%
溶剂/溶解度	DMSO 10mM, need ultrasonic and warm at 37℃; Water insoluble
溶液配制	5mg加入1.167ml DMSO，或者每4.28mg加入1ml DMSO，配制成10mM溶液，超声并37℃水浴处理。

生物信息:

产品描述	MLN-4760 is an effective and selective inhibitor of human ACE2 (IC50, 0.44 nM). It also has excellent selectivity (>5000-fold) versus related enzymes including human testicular ACE (IC50>100 μM) and bovine carboxypeptidase A (CPDA; IC50, 27 μM). MLN-4760 also enables to study the effect of reduced ACE2 activity on the lung’s susceptibility for Coronavirus disease (COVID) related acute respiratory distress syndrome (ARDS).
信号通路	Anti COVID-19; Antimicrobial Signaling; Metabolic Enzyme/Protease
靶点	Human ACE2	Bovine carboxypeptidase A	Human testicular ACE	-	-
IC50/EC50	0.44 nM	27 μM	>100 μM	-	-
体外研究	MLN-4760 is a potent and selective human ACE2 inhibitor (IC50, 0.44 nM), with excellent selectivity (>5000-fold) versus related enzymes human testicular ACE (IC50, >100 μM) and bovine carboxypeptidase A (CPDA; IC50, 27 μM). MLN-4760 effectively quenches cleavage of the 7-Mca-YVADAPK(Dnp) in rhACE2. MLN-4760 shows pIC50 at rhACE2 of 8.5±0.1 and at rhACE of 4.4±0.2. MLN-4760 also shows pIC50 at rhACE2 of 4.7±0.1, 6.9±0.1 and at ACE of 4.4±0.1, 6.2±0.1 in murine heart and mononuclear cells (MNCs), resepctively.
体内研究	MLN-4760 (100 μM, intracerebroventricular infusion for five days) significantly worsens neurological function at 4 h and 3 d post-stroke without significantly increasing infarct volume.
临床实验	-
特征	-

相关实验数据(此数据来自于公开文献，并不保证其有效性)：

酶活性检测实验
方法	N/A

细胞实验
细胞系	-
浓度	-
处理时间	-
方法	-

动物实验
动物模型	-
配制	1. Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% saline Solubility: ≥ 5 mg/mL (11.67 mM); Clear solution 2. Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in saline) Solubility: ≥ 5 mg/mL (11.67 mM); Clear solution 3. Add each solvent one by one: 10% DMSO 90% corn oil Solubility: ≥ 5 mg/mL (11.67 mM); Clear solution
剂量	-
给药方式	-

参考文献：

1. Dales NA, et al. Substrate-based design of the first class of angiotensin-converting enzyme-related carboxypeptidase (ACE2) inhibitors. J Am Chem Soc. 2002 Oct 9;124(40):11852-3.

2. Joshi S, et al. Angiotensin converting enzyme versus angiotensin converting enzyme-2 selectivity of MLN-4760 and DX600 in human and murine bone marrow-derived cells. Eur J Pharmacol. 2016 Mar 5;774:25-33.

3. Bennion DM, et al. Activation of the Neuroprotective Angiotensin-Converting Enzyme 2 in Rat Ischemic Stroke. Hypertension. 2015 Jul;66(1):141-8.

包装清单：

产品编号	产品名称	包装
SF1197-10mM	MLN-4760 (ACE2抑制剂)	10mM×0.2ml
SF1197-5mg	MLN-4760 (ACE2抑制剂)	5mg
SF1197-25mg	MLN-4760 (ACE2抑制剂)	25mg
SF1197-100mg	MLN-4760 (ACE2抑制剂)	100mg
－	说明书	1份