MLN-4760,305335-31-3

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MLN-4760

CAS No. : 305335-31-3

MCE 国际站：MLN-4760

产品活性：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)。

研究领域：Metabolic Enzyme/Protease

作用靶点：Angiotensin-converting Enzyme (ACE)

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.

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.

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