MLN-4760 - 99%, high purity , CAS No.305335-31-3, Inhibitor of Angiotensin-converting enzyme 2

Item Number

M414282

• Synonyms: (2S)-2-{[(1S)-1-carboxy-2-{1-[(3,5-dichlorophenyl)methyl]-1H-imidazol-5-yl}ethyl]amino}-4-methylpentanoic acid | AKOS040742161 | MS-27570 | UNII-4LD0ZHV25K | (S)-2-(((S)-1-carboxy-2-(1-(3,5-dichlorobenzyl)-1H-imidazol-5-yl)ethyl)amino)-4-methylpentanoic a
• Specifications & Purity: Moligand™, ≥99%
• Biochemical and Physiological Mechanisms: MLN-4760 (compound 16) is a potent and selective inhibitor of human angiotensin-converting enzyme 2 (ACE2) with IC50 of 0.44 nM. MLN-4760 also inhibits bovine carboxypeptidase A (CPDA) with IC50 of 27 μM.
• Storage Temp: Protected from light,Store at -20°C,Argon charged
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Inhibitor of Angiotensin-converting enzyme 2

Product Description

ACE2 (Cell-free assay); CPDA (Cell-free assay) 0.44 nM; 27 μM

In vitro

conversion from angiotensin II to angiotensin-(1–7) by mouse ACE2 is blocked by MLN-4760 (10 μM). MLN-4760 inhibits both human and mouse ACE2 activity. In huMNCs, MLN-4760-B (an isomer of MLN-4760) detects 63% ACE2 with 28-fold selectivity over ACE. In huCD34+ cells, MLN-4760-B detects 38% of ACE2 activity with 63-fold selectivity. In mu-heart and muMNCs, MLN-4760-B is 100- and 228-fold selective for ACE2, respectively. In muLin- cells, MLN-4760-B detects 25% ACE2 activity with a pIC50 of 6.3. The racemic mixture and MLN-4760-A shows lower efficacy and poor selectivity for ACE2 in MNCs and mu-heart.

In vivo

MLN-4760 blocks ACE2 activity, thus significantly reverses the elevation of carotid Ang-(1-7) level and the decline of carotid Ang II level induced by NaHS in mice. The anti-atherosclerotic property of NaHS is also significantly abolished by treatment with MLN-4760.

Cell Research(from reference)

Cell lines：mononuclear cells (MNCs), huCD34+ cells, mu-lineage-depleted (muLin-) cells 

Concentrations：0.01 nM to 300 μM 

Incubation Time：1 h, 4 h