[CAS NO. 305335-31-3]  MLN-4760

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PRODUCTS SPECIFICATIONS [305335-31-3]

Store
Catalog
SLK-S8940
Brand
Selleck
CAS
305335-31-3

DESCRIPTION [305335-31-3]

Overview

MDLMFCD30532572
Molecular Weight428.31
Molecular FormulaC19H23Cl2N3O4
SMILESO=C(O)[C@H](CC1=CN=CN1CC2=CC(Cl)=CC(Cl)=C2)N[C@H](C(O)=O)CC(C)C

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.3348 mL11.6738 mL23.3476 mL
5 mM0.4670 mL2.3348 mL4.6695 mL
10 mM0.2335 mL1.1674 mL2.3348 mL
50 mM0.0467 mL0.2335 mL0.4670 mL

Description

MLN-4760 (compound 16) is a potent and selective inhibitor of human with IC50 of 0.44 nM. MLN-4760 also inhibits with IC50 of 27 μM.

Targets

ACE2 [1]
(Cell-free assay)
CPDA [1]
(Cell-free assay)
0.44 nM27 μM

In vitro

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.