MLN-4760
目录号: PL14793 纯度: ≥99%
CAS No. :305335-31-3
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中文名称
MLN-4760
英文名称
MLN-4760
英文别名
L-Histidine,N-[(1S)-1-carboxy-3-methylbutyl]-3-[(3,5-dichlorophenyl)methyl]-;(2S)-2-[[(1S)-1-carboxy-2-[3-[(3,5-dichlorophenyl)methyl]imidazol-4-yl]ethyl]amino]-4-methylpentanoic acid;MLN-4760;MLN4760;ORE1001;MLN 4760;GL1001;4LD0ZHV25K;(2S)-2-[[(2S)-3-[3-[(3,5-dichlorophenyl)methyl]imidazol-4-yl]-1-hydroxy-1-oxopropan-2-yl]amino]-4-methylpentanoic acid;(S,S)-2-{1-CARBOXY-2-[3-(3,5-DICHLORO-BENZYL)-3H-IMIDAZOL-4-YL]-ETHYLAMINO}-4-METHYL-PENTANOIC ACID;N-[(1s)-1-carboxy-3-methylbutyl]-3-(3,5-dichlorobenzyl)-l-histidine;XX5;GTPL7866;BDBM21489
Cas No.
305335-31-3
分子式
C19H23Cl2N3O4
分子量
428.31
包装储存
4°C, stored under nitrogen, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
产品详情
MLN-4760 是一种有效、选择性的人 ACE2 抑制剂,IC50 值为 0.44 nM,对其选择性是对其他相关蛋白的 5000 多倍,包括人睾丸 ACE (IC50,>100 μM) 和牛 carboxypeptidase A (IC50,27 μM)。
生物活性
MLN-4760 is a potent and selective human ACE2 inhibitor (IC 50 , 0.44 nM), with excellent selectivity (>5000-fold) versus related enzymes including human testicular ACE (IC 50 , >100 μM) and bovine carboxypeptidase A (CPDA; IC 50 , 27 μM).
性状
Solid
IC50 & Target[1][2]
IC50: 0.44 nM (Human ACE2), 27 μM (Bovine carboxypeptidase A)
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, stored under nitrogen, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
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.
溶解度数据
In Vitro: DMSO : ≥ 50 mg/mL (116.74 mM)H2O : < 0.1 mg/mL (ultrasonic;warming;adjust pH to 11 with NaOH;heat to 60°C) (insoluble)
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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