Name | MLN-4760 |
Synonyms | MLN-4760 ((S)-1-carboxy-2-(1-(3,5-dichlorobenzyl)-1H-imidazol-5-yl)ethyl)-L-leucine L-Histidine, N-[(1S)-1-carboxy-3-methylbutyl]-3-[(3,5-dichlorophenyl)methyl]- |
CAS | 305335-31-3 |
Molecular Formula | C19H23Cl2N3O4 |
Molar Mass | 428.31 |
Solubility | DMSO : 100 mg/mL (233.48 mM; Need ultrasonic) |
Storage Condition | -20℃ |
Use | MLN-4760 is an effective and selective human ACE2 inhibitor with an IC50 value of 0.44 nM, which is more than 5000 times more selective than other related proteins, including human testicular ACE (IC50,>100 μM) and bovine carboxypeptidase A (IC50,27 μM). |
Target | Human ACE2; Bovine carboxypeptidase A |
In vitro study | MLN-4760 is a potent and selective human ACE2 inhibitor (IC 50 , 0.44 nM), with excellent selectivity (>5000-fold) versus related enzymes human testicular ACE (IC 50 , >100 μM) and bovine carboxypeptidase A (CPDA; IC 50 , 27 μM). MLN-4760 effectively quenches cleavage of the 7-Mca-YVADAPK(Dnp) in rhACE2. MLN-4760 shows pIC 50 at rhACE2 of 8.5±0.1 and at rhACE of 4.4±0.2. MLN-4760 also shows pIC 50 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 study | 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. |
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 |
5 mM | 0.047 ml | 0.233 ml | 0.467 ml |
biological activity | MLN-4760 (compound 16) is a potent, selective human angiotensin-converting enzyme 2 (ACE2) the IC50 value of the inhibitor was 0.44 nM. MLN-4760 also inhibited bovine carboxypeptidase A (CPDA) with an IC50 value of 27 μm. |
Target | Value |
ACE2 (Cell-free assay) | 0.44 nM |
CPDA (Cell-free assay) | 27 μM |