MLN-4760

For research use only.

Catalog No.S8940

MLN-4760 Chemical Structure

CAS No. 305335-31-3

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.

Purity & Quality Control

Choose Selective ACE Inhibitors

Biological Activity

Description 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.
Targets
ACE2 [1]
(Cell-free assay)
CPDA [1]
(Cell-free assay)
0.44 nM 27 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.[3] 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.[4]

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.[2]

Protocol

Cell Research:

[4]

- Collapse
  • 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
  • Method:

    In the case of cell lysates, 10 μg of total protein is assayed for activity in a buffer with the following composition: 50mM MES (4-morpholineethanesulphonic acid), 300mM NaCl, 10μM ZnCl2 and 0.01% Triton X-100, pH 6.5. Reaction is initiated by the addition of 5×10-5 M substrate. Where applicable, recombinant enzymes are used at a concentration of 0.01 μg per reaction. The fluorescence measurements are performed in the black microtiter plates in a total volume of 100 μl. The plates are read using a fluorescence plate reader SpectraMax M5 at an excitation wavelength 320 nm and emission wavelength 405 nm Fluorescence resulting from the substrate hydrolysis increased with time, and achieved maximum by 1 h with recombinant enzyme however with cell/tissue lysates the maximum fluorescence is observed by 4 h of incubation. Therefore fluorescence recorded at 1 and 4 h of reaction time is taken for calculation of percent enzyme inhibition, when using recombinant enzymes and cell/tissue lysates, respectively. ACE2 activity is defined as the ACE2 inhibitor-sensitive fluorescence and ACE activity is defined as the ACE inhibitor, captopril-sensitive fluorescence, and are expressed as percent inhibition. Unless specified, MLN4760 is used in concentration ranging from 0.01 nM to 300 μM.


    (Only for Reference)
Animal Research:

[2]

- Collapse
  • Animal Models: C57BL/6J male apoE−/− mice
  • Dosages: 0.5 mg/kg
  • Administration: IP
    (Only for Reference)

Solubility (25°C)

In vitro Water 86 mg/mL (200.78 mM)
DMSO Insoluble
Ethanol '''10 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 428.31
Formula
C19H23Cl2N3O4
CAS No. 305335-31-3
Storage powder
in solvent
Synonyms N/A
Smiles CC(C)CC(C(=O)O)NC(CC1=CN=CN1CC2=CC(=CC(=C2)Cl)Cl)C(=O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field
Tags: buy MLN-4760 | MLN-4760 supplier | purchase MLN-4760 | MLN-4760 cost | MLN-4760 manufacturer | order MLN-4760 | MLN-4760 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID