MLN-4760CAS号: 305335-31-3分子式: C19H23Cl2N3O4分子量: 428.31描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
MLN-4760 is an angiotensin-converting (ACE2) inhibitor(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).
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纯度 |
98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
可溶性/溶解性 |
DMSO:199 mg/mL(464.62 mM)
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生物活性 | |
靶点 |
Human ACE2:0.44 nM (IC50), Bovine carboxypeptidase A:27 μM (IC50)
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In vitro(体外研究) |
MLN-4760 displays 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 an ACE of 4.4±0.1, 6.2±0.1 in murine heart and mononuclear cells (MNCs), respectively. MLN-4760 potently quenches the cleavage of the 7-Mca-YVADAPK(Dnp) in rhACE2[2].
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In vivo(体内研究) |
MLN-4760 (100 μM, intracerebroventricular infusion for five days) obviously worsens neurological function at 4 h and 3 d post-stroke. However, without obviously increasing infarct volume[3].
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