货号	规格	价格	上海	北京	珠海	重庆	武汉
S89112-1mg买3赠1	99.70%	￥390.00 S89112-1mg ￥390.00 现货（买3赠1）	5 5	-	-	-	-
S89112-5mg买3赠1	99.70%	￥990.00 S89112-5mg ￥990.00 现货（买3赠1）	2 0 2	-	-	-	-
S89112-10mg	≥95%	￥1690.00 S89112-10mg ￥1690.00 2-3天	0 货期：2-3天	-	-	-	-
S89112-50mg	≥95%	￥5590.00 S89112-50mg ￥5590.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

MLN-4760 is a potent and selective human ACE2 inhibitor (IC50, 0.44 nM), with excellent selectivity (>5000-fold) versus related enzymes including human testicular ACE (IC50, >100 μM) and bovine carboxypeptidase A (CPDA; IC50, 27 μM).

靶点：

IC50: 0.44 nM (Human ACE2), 27 μM (Bovine carboxypeptidase A);RAAS

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。

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.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.335 ml	11.674 ml	23.348 ml
5 mM	0.467 ml	2.335 ml	4.67 ml
10 mM	0.233 ml	1.167 ml	2.335 ml
50 mM	0.047 ml	0.233 ml	0.467 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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