Cat. No.: HY-19414

MLN-4760

Name: MLN-4760
Brand: MedChemExpress
SKU: HY-19414
Price: 140.00 USD
Availability: InStock
Rating: 5 (26 reviews)

26 Cited Publications

Customer Review

Based on 26 publication(s) in Google Scholar

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.

Purity : 99.78%
CAS No.: 305335-31-3
Formula: C₁₉H₂₃Cl₂N₃O₄
Molecular Weight:428.31

Storage:

4°C, stored under nitrogen, away from moisture

* In solvent : -80°C, 2 years; -20°C, 1 year (stored under nitrogen, away from moisture)

MLN-4760 Chemical Structure

CAS No.: 305335-31-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (26)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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.

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.

Chemical Information

CAS No. 305335-31-3
Appearance Solid
Molecular Weight 428.31
Formula C₁₉H₂₃Cl₂N₃O₄
Color 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, 2 years; -20°C, 1 year (stored under nitrogen, away from moisture)

Publications (26)

All Bio/Physico-chemical AssayIn Vivo Efficacy StudyFlow CytometryRT-PCR

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Journal Impact Factor

Acta Pharm Sin B

Identifying potential anti-COVID-19 pharmacological components of traditional Chinese medicine Lianhuaqingwen capsule based on human exposure and ACE2 biochromatography screening. [Abstract]

2021 Jan;11(1):222-236. PMID: 33072499

MLN-4760 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2021 Jan;11(1):222-236. [Abstract]

SPR sensorgram and equilibrium dissociation constant fitting curve for the binding of MLN-4760 (0.024-50 μM; 120-s association and 120-s dissociation) to recombinant human ACE2 protein. MLN-4760 showed strong binding affinity for ACE2, with a K_D value of 0.029 μM.
J Biomed Sci

The ACE2 decoy receptor can overcome immune escape by rapid mutating SARS-CoV-2 variants and reduce cytokine induction and clot formation. [Abstract]

2025 Jun 26;32(1):59. PMID: 40571942
Sci Adv

2026 Aug 7;12(32):eaee2515. PMID: 42566544
Antioxidants (Basel)

MLN-4760 Induces Oxidative Stress without Blood Pressure and Behavioural Alterations in SHRs: Roles of Nfe2l2 Gene, Nitric Oxide and Hydrogen Sulfide. [Abstract]

2022 Dec 1;11(12):2385. PMID: 36552591

MLN-4760 purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2022 Dec 1;11(12):2385. [Abstract]

Brainstem conjugated diene content in spontaneously hypertensive rats after 14 days of MLN-4760 administration (1 mg/kg/day; s.c.; continuous infusion). MLN-4760 significantly increased brainstem conjugated diene content.

MLN-4760 purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2022 Dec 1;11(12):2385. [Abstract]

Brainstem mRNA expression of Sod1, Sod2, Gpx4, Hmox1, and Nfe2l2 in spontaneously hypertensive rats after 14 days of MLN-4760 administration (1 mg/kg/day; s.c.; continuous infusion). MLN-4760 significantly increased the expression of these genes.
ACS Appl Mater Interfaces

Conditional Cell-Penetrating Peptide Exposure as Selective Nanoparticle Uptake Signal. [Abstract]

2024 Jul 24;16(29):37734-37747. PMID: 39010308
Crit Care Med

Association of Active Renin Content With Mortality in Critically Ill Patients: A Post hoc Analysis of the Vitamin C, Thiamine, and Steroids in Sepsis Trial. [Abstract]

2024 Mar 1;52(3):441-451. PMID: 37947484
Clin Sci

Higher circulating ACE2 and DPP3 but reduced ACE and angiotensinogen in hyperreninemic sepsis patients. [Abstract]

2025 Jan 15;139(1):43-53. PMID: 39699964
Int J Pharm

Ectoenzymes as Promising Cell Identification Structures for the High Avidity Targeting of Polymeric Nanoparticles. [Abstract]

2023 Nov 25:647:123453. PMID: 37783283

MLN-4760 purchased from MedChemExpress. Usage Cited in: Int J Pharm. 2023 Nov 25:647:123453. [Abstract]

Flow cytometric analysis of MLN-NP binding/uptake over time in HEK293T-ACE2 target cells in the presence of free MLN-4760 (200 μM; 15-min pretreatment followed by co-incubation with nanoparticles for up to 120 min).

MLN-4760 purchased from MedChemExpress. Usage Cited in: Int J Pharm. 2023 Nov 25:647:123453. [Abstract]

Residual ACE2 activity in HEK293T-ACE2 cells after exposure to free MLN-4760 (200 μM; 1 h), as measured using a fluorogenic ACE2 substrate. Free MLN-4760 in excess served as positive control for the complete enzyme inhibition.
Pharm Biol

Fraxinol attenuates LPS-induced acute lung injury by equilibrating ACE-Ang II-AT1R and ACE2-Ang (1-7)-Mas and inhibiting NLRP3. [Abstract]

2022 Dec;60(1):979-989. PMID: 35588103
Infect Dis Ther

Computational and Experimental Studies Reveal That Thymoquinone Blocks the Entry of Coronaviruses Into In Vitro Cells. [Abstract]

2021 Mar;10(1):483-494. PMID: 33532909
Invest Ophthalmol Vis Sci

Senolytic Treatment Alleviates Corneal Allograft Rejection Through Upregulation of Angiotensin-Converting Enzyme 2 (ACE2). [Abstract]

2025 Feb 3;66(2):15. PMID: 39913165
Biol Res

The effect of zofenopril on the cardiovascular system of spontaneously hypertensive rats treated with the ACE2 inhibitor MLN-4760. [Abstract]

2023 Oct 25;56(1):55. PMID: 37875978
Chem Biol Interact

Mechanism of ferroptosis in hypoxia-induced pulmonary vascular remodeling in hypoxia pulmonary hypertension: a study based on the ACE2-Ang-(1-7)-Mas axis. [Abstract]

2025 Sep 5:418:111596. PMID: 40466901
Sci Rep

Reduced circulating 20-hydroxyeicosatetraenoic acid and ACE2 in acute coronary syndrome with exploratory cell-based observations. [Abstract]

2026 Jun 10. PMID: 42270785
J Cell Mol Med

Geraniin Alleviates Mouse Laser-Induced Choroidal Neovascularisation by Inhibiting Choroidal Endothelial Cell ACE2/Ang-(1-7)/MasR/IL-10 Pathway. [Abstract]

2024 Dec;28(23):e70228. PMID: 39622780
Cell Signal

The Apelin-APJ axis alleviates LPS-induced pulmonary fibrosis and endothelial mesenchymal transformation in mice by promoting Angiotensin-Converting Enzyme 2. [Abstract]

2022 Oct:98:110418. PMID: 35882286
Biomedicines

Angiotensin System Modulations in Spontaneously Hypertensive Rats and Consequences on Erythrocyte Properties; Action of MLN-4760 and Zofenopril. [Abstract]

2021 Dec 14;9(12):1902. PMID: 34944718
Noncoding RNA

CRISPR/CasRx-Mediated RNA Knockdown Reveals That ACE2 Is Involved in the Regulation of Oligodendroglial Cell Morphological Differentiation. [Abstract]

2022 Jun 6;8(3):42. PMID: 35736639
J Virol

Differential expression of viral entry protein neuropilin 1 (NRP1) and neuropilin 2 (NRP2) in fatal COVID-19. [Abstract]

2025 Oct 29:e0138425. PMID: 41159753
Front Biosci (Landmark Ed)

ACE2 Alleviates Endoplasmic Reticulum Stress and Protects against Pyroptosis by Regulating Ang1-7/Mas in Ventilator-Induced Lung Injury. [Abstract]

2024 Sep 24;29(9):334. PMID: 39344337
J Endocrinol Invest

Dapagliflozin ameliorates high glucose-induced epithelial-mesenchymal transition via up-regulating ACE2 mediated by EZH2 in diabetic nephropathy. [Abstract]

2025 Jul 14. PMID: 40658352
Life

Effects of Taxifolin in Spontaneously Hypertensive Rats with a Focus on Erythrocyte Quality. [Abstract]

2022 Dec 7;12(12):2045. PMID: 36556410
Toxicol Appl Pharmacol

Saikosaponin D protects against isoproterenol-induced kidney injury in rats by regulating the intrarenal renin-angiotensin system. [Abstract]

2026 Mar 27:511:117802. PMID: 41903810
Biomed Res Int

Characterization of the Modulatory Effect of Hydroxychloroquine on ACE2 Activity: New Insights in relation to COVID-19. [Abstract]

2021 Jul 23:2021:6614000. PMID: 34337036
bioRxiv

2025 Oct 26.
bioRxiv

Development of a mutant aerosolized ACE2 that neutralizes SARS-CoV-2 in vivo. [Abstract]

2023 Oct 5:2023.09.26.559550. PMID: 37808801

Solvent & Solubility

In Vitro:

DMSO : 8.33 mg/mL (19.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3348 mL

11.6738 mL

23.3476 mL

5 mM

0.4670 mL

2.3348 mL

4.6695 mL

10 mM

0.2335 mL

1.1674 mL

2.3348 mL

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, 2 years; -20°C, 1 year (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Dales NA, et al. Substrate-based design of the first class of angiotensin-converting enzyme-related carboxypeptidase (ACE2) inhibitors. J Am Chem Soc. 2002 Oct 9;124(40):11852-3. [Content Brief]

[2]. Joshi S, et al. Angiotensin converting enzyme versus angiotensin converting enzyme-2 selectivity of MLN-4760 and DX600 in human and murine bone marrow-derived cells. Eur J Pharmacol. 2016 Mar 5;774:25-33. [Content Brief]

[3]. Bennion DM, et al. Activation of the Neuroprotective Angiotensin-Converting Enzyme 2 in Rat Ischemic Stroke. Hypertension. 2015 Jul;66(1):141-8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	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

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MLN-4760

Publications Citing Use of MedChemExpress (MCE) MLN-4760