MLN-4760
Based on 25 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
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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)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) MLN-4760
More- Acta Pharm Sin B. 2021 Jan;11(1):222-236. [Abstract]
- J Biomed Sci. 2025 Jun 26;32(1):59. [Abstract]
- ACS Appl Mater Interfaces. 2024 Jul 24;16(29):37734-37747. [Abstract]
- Clin Sci. 2025 Jan 15;139(1):43-53. [Abstract]
- Antioxidants (Basel). 2022 Dec 1;11(12):2385. [Abstract]
- Crit Care Med. 2024 Mar 1;52(3):441-451. [Abstract]
- Chem Biol Interact. 2025 Jun 2:111596. [Abstract]
- Infect Dis Ther. 2021 Mar;10(1):483-494. [Abstract]
- Int J Pharm. 2023 Nov 25:647:123453. [Abstract]
- Pharm Biol. 2022 Dec;60(1):979-989. [Abstract]
- Invest Ophthalmol Vis Sci. 2025 Feb 3;66(2):15. [Abstract]
- Biol Res. 2023 Oct 25;56(1):55. [Abstract]
- J Cell Mol Med. 2024 Dec;28(23):e70228. [Abstract]
- Sci Rep. 2026 Jun 10. [Abstract]
- Biomedicines. 2021 Dec 14;9(12):1902. [Abstract]
- J Virol. 2025 Oct 29:e0138425. [Abstract]
- Cell Signal. 2022 Oct:98:110418. [Abstract]
- J Endocrinol Invest. 2025 Jul 14. [Abstract]
- Toxicol Appl Pharmacol. 2026 Mar 27:511:117802. [Abstract]
- Life. 2022 Dec 7;12(12):2045. [Abstract]
- Front Biosci (Landmark Ed). 2024 Sep 24;29(9):334. [Abstract]
- Noncoding RNA. 2022 Jun 6;8(3):42. [Abstract]
- Biomed Res Int. 2021 Jul 23:2021:6614000. [Abstract]
- bioRxiv. 2025 Oct 26.
- bioRxiv. 2023 Oct 5:2023.09.26.559550. [Abstract]
Biological Activity
IC50: 0.44 nM (Human ACE2), 27 μM (Bovine carboxypeptidase A)[1]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 305335-31-3
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Appearance Solid
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Molecular Weight 428.31
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Formula C19H23Cl2N3O4
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Color White to light yellow
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SMILES
O=C(O)[C@H](CC1=CN=CN1CC2=CC(Cl)=CC(Cl)=C2)N[C@H](C(O)=O)CC(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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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 (25)
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Journal Impact Factor
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Most Recent
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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 -
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 -
ACS Appl Mater Interfaces
2024 Jul 24;16(29):37734-37747. PMID: 39010308 -
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 -
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 -
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 -
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 Jun 2:111596. PMID: 40466901 -
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 -
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 -
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 -
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 -
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 -
Sci Rep
Reduced circulating 20-hydroxyeicosatetraenoic acid and ACE2 in acute coronary syndrome with exploratory cell-based observations. [Abstract]2026 Jun 10. PMID: 42270785 -
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 -
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 -
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 -
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 -
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 -
Life
Effects of Taxifolin in Spontaneously Hypertensive Rats with a Focus on Erythrocyte Quality. [Abstract]2022 Dec 7;12(12):2045. PMID: 36556410 -
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 -
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 -
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 -
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bioRxiv
2023 Oct 5:2023.09.26.559550. PMID: 37808801
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (stored under nitrogen, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (282 KB)
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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)
- Portuguese - PT (393 KB)
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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]
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, 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.
| 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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