MLN-4760 (C007B-231130)

ACE2 (Cell-free assay); CPDA (Cell-free assay) 0.44 nM; 27 μMIn vitroconversion 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 vivoMLN-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. Specification: 0.99 Molecular Formula: C19H23Cl2N3O4 Molecular Weight: 428.31 PubChem CID: 448281 Isomeric SMILES: CC(C)C[C@@H](C(=O)O)N[C@@H](CC1=CN=CN1CC2=CC(=CC(=C2)Cl)Cl)C(=O)O Related Documents: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/M414282-SCI_013f22c35fec0e771265d03ddff60bbd.pdf