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

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).

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MLN-4760 Chemical Structure

MLN-4760 Chemical Structure

CAS No. : 305335-31-3

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1 mg USD 160 In-stock
5 mg USD 400 In-stock
10 mg USD 640 In-stock
25 mg USD 1150 In-stock
50 mg USD 1700 In-stock
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Based on 14 publication(s) in Google Scholar

Other Forms of MLN-4760:

MLN-4760 Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

MLN-4760 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

428.31

Formula

C19H23Cl2N3O4
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(O)[C@H](CC1=CN=CN1CC2=CC(Cl)=CC(Cl)=C2)N[C@H](C(O)=O)CC(C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (233.48 mM; Need ultrasonic)

DMSO : 50 mg/mL (116.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3348 mL 11.6738 mL 23.3476 mL
5 mM 0.4670 mL 2.3348 mL 4.6695 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.84 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.84 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.93%

COA (258 KB) HNMR (212 KB) LCMS (130 KB)

Handling Instructions (2659 KB)
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.3348 mL 11.6738 mL 23.3476 mL 58.3689 mL
5 mM 0.4670 mL 2.3348 mL 4.6695 mL 11.6738 mL
10 mM 0.2335 mL 1.1674 mL 2.3348 mL 5.8369 mL
15 mM 0.1557 mL 0.7783 mL 1.5565 mL 3.8913 mL
20 mM 0.1167 mL 0.5837 mL 1.1674 mL 2.9184 mL
25 mM 0.0934 mL 0.4670 mL 0.9339 mL 2.3348 mL
30 mM 0.0778 mL 0.3891 mL 0.7783 mL 1.9456 mL
40 mM 0.0584 mL 0.2918 mL 0.5837 mL 1.4592 mL
50 mM 0.0467 mL 0.2335 mL 0.4670 mL 1.1674 mL
60 mM 0.0389 mL 0.1946 mL 0.3891 mL 0.9728 mL
80 mM 0.0292 mL 0.1459 mL 0.2918 mL 0.7296 mL
100 mM 0.0233 mL 0.1167 mL 0.2335 mL 0.5837 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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MLN-4760 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MLN-4760305335-31-3MLN4760MLN 4760Angiotensin-converting Enzyme (ACE)Inhibitorinhibitorinhibit

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