1. Metabolic Enzyme/Protease
  2. Angiotensin-converting Enzyme (ACE)
  3. MLN-4760

MLN-4760 

Cat. No.: HY-19414
Handling Instructions

MLN-4760 is a potent and selective human ACE2 inhibitor (IC50, 0.44 nM), with excellent selectivity (>5000-fold) versus related enzymes including human testicular ACE (IC50, >100 μM) and bovine carboxypeptidase A (CPDA; IC50, 27 μM).

For research use only. We do not sell to patients.

MLN-4760 Chemical Structure

MLN-4760 Chemical Structure

CAS No. : 305335-31-3

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Description

MLN-4760 is a potent and selective human ACE2 inhibitor (IC50, 0.44 nM), with excellent selectivity (>5000-fold) versus related enzymes including human testicular ACE (IC50, >100 μM) and bovine carboxypeptidase A (CPDA; IC50, 27 μM).

IC50 & Target

IC50: 0.44 nM (Human ACE2), 27 μM (Bovine carboxypeptidase A)[1]

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)[1]. 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[2].

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[3].

Molecular Weight

428.31

Formula

C₁₉H₂₃Cl₂N₃O₄

CAS No.

305335-31-3

SMILES

O=C(O)[[email protected]](CC1=CN=CN1CC2=CC(Cl)=CC(Cl)=C2)N[[email protected]](C(O)=O)CC(C)C

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Animal Administration
[3]

Rats[3]
In a related experiment to evaluate the role of central ACE2 in stroke, randomly assigned rats (n = 16) are treated centrally for five days prior to and three days after stroke with the ACE2 inhibitor MLN-4760 (100 μM infused at a rate of 0.5 μL/h) or sterile saline (0.9%) via intracerebroventricular infusion. Following endothelin-1 MCAO, neurological function is assessed at 4 h, 1 d, and 3 d, and brains are harvested at 3 d post-stroke for infarct volume analysis as above[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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