ChemicalBook > CAS DataBase List > MLN-4760

MLN-4760

Product Name: MLN-4760
CAS No.: 305335-31-3
Chemical Name: MLN-4760
Synonyms: MLN-4760;MLN-4760 ，S8940;ACE2 Inhibitor, MLN-4760;MLN-4760 Chemical Structure;((S)-1-carboxy-2-(1-(3,5-dichlorobenzyl)-1H-imidazol-5-yl)ethyl)-L-leucine;L-Histidine, N-[(1S)-1-carboxy-3-methylbutyl]-3-[(3,5-dichlorophenyl)methyl]-;inhibit,Angiotensin-converting Enzyme (ACE),MLN 4760,Inhibitor,MLN-4760,MLN4760;(2S)-2-{[(1S)-1-carboxy-2-{1-[(3,5-dichlorophenyl)methyl]-1H-imidazol-5-yl}ethyl]amino}-4-methylpentanoic acid
CBNumber: CB64845021
Molecular Formula: C19H23Cl2N3O4
Formula Weight: 428.31
MOL File: 305335-31-3.mol

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MLN-4760 Property

storage temp.: Store at -20°C
solubility: DMSO: soluble
form: A solid
color: Off-white to light yellow
InChIKey: NTCCRGGIJNDEAB-IRXDYDNUSA-N
SMILES: C(O)(=O)[C@H](CC1N(CC2=CC(Cl)=CC(Cl)=C2)C=NC=1)N[C@H](C(O)=O)CC(C)C

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H312Harmful in contact with skin

H332Harmful if inhaled

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P330Rinse mouth.

P362Take off contaminated clothing and wash before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: 5.30616
Product name: ACE2 Inhibitor, MLN-4760
Purity: ≥97% (HPLC), powder, Calbiochem?
Packaging: 2MG
Price: $273
Updated: 2023/01/07

ChemScene

Product number: CS-0015513
Product name: MLN-4760
Purity: 99.93%
Packaging: 1mg
Price: $200
Updated: 2021/12/16

ChemScene

Product number: CS-0015513
Product name: MLN-4760
Purity: 99.93%
Packaging: 5mg
Price: $480
Updated: 2021/12/16

ChemScene

Product number: CS-0015513
Product name: MLN-4760
Purity: 99.93%
Packaging: 10mg
Price: $800
Updated: 2021/12/16

ChemScene

Product number: CS-0015513
Product name: MLN-4760
Purity: 99.93%
Packaging: 25mg
Price: $1700
Updated: 2021/12/16

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MLN-4760 Chemical Properties,Usage,Production

Uses

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).

Definition

ChEBI: MLN-4760 is a L-histidine derivative that is L-histidine in which a hydrogen of the primary amino group is substituted by a (1S)-1-carboxy-3-methylbutyl group and the ring NH group is substituted by a 3,5-dichlorobenzyl group. It is a potent and selective human angiotensin-converting enzyme 2 (ACE2) inhibitor (IC50 = 0.44 nM) which was in clinical development for the treatment of ulcerative colitis. It has a role as an anti-inflammatory agent and an EC 3.4.17.23 (angiotensin-converting enzyme 2) inhibitor. It is a L-histidine derivative, a dichlorobenzene and a L-leucine derivative.

Biological Activity

MLN-4760 is bioavailable and exhibits far greater selectivity for carboxypeptidase (IC50 = 0.44 nM against 50 pM human ACE2; [ZnCl2] = 10 μM, [MCA-APK(DNP)] = 50 μM) over bovine carboxypeptidase A or ACE peptidyldipeptidase activity (IC50 = 27 μM and >100 μM against 0.5 nM bovine CPDA and 1 nM porcine ACE, respectively; [Substrate] = 50 μM) and porcine ACE (IC50 = 27 and >100 μM, respectively). This reversible ACE2 inhibitor binds to the active site zinc with high-affinity and emulates the transition state during peptide hydrolysis. It reduces serum and kidney ACE 2 activity and abolishes angiotensin II-induced hypertension in mice. MLN-4760 selectively blocks angiotensin (ANG-(1-7)) formation in ACE2 wild type (WT) mice subjected to low ANG II concentrations (<0.1 μM), but at higher ANG II concentrations it does not affect ANG -(1-7) levels in mice. This ACE2 inhibitor enhances tumor necrosis factor (TNF) (10 pg/mL) stimulated expression of proinflammatory cytokines in murine endothelial cells, (1 μM using SVEC-40 line and primary aorta endothelial cultures) in vitro. MLN-4760 is widely employed for studying ACE2 involvement in kidney, cardiovascular and inflammatory bowel diseases via drinking water (10 mg/kg/d), i.v. (0.1 mg/kg), and s.c. (30 mg/kg/d to 300 mg/kg/12 h) injection in rats and mice, in vivo. The inhibitor leucine moiety is shown to simultaneously target ACE2 substrate S1 pocket with its isobutyl group and active site zinc via its carboxylate, while the compoundμs 3,5-dichlorobenzyl group effectively occupy S1μ subsite.
MLN-4760 also enables to study the effect of reduced ACE2 activity on the lung′s susceptibility for Coronavirus disease (COVID) related acute respiratory distress syndrome (ARDS).

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].

storage

Store at -20°C

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. DOI:10.1021/ja0277226
[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. DOI:10.1016/j.ejphar.2016.01.007
[3] Bennion DM, et al. Activation of the Neuroprotective Angiotensin-Converting Enzyme 2 in Rat Ischemic Stroke. Hypertension. 2015 Jul;66(1):141-8. DOI:10.1161/HYPERTENSIONAHA.115.05185

MLN-4760 Preparation Products And Raw materials

Raw materials

Preparation Products

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MLN-4760 Suppliers

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View Lastest Price from MLN-4760 manufacturers

ZHENGZHOU JIUYI TIME NEW MATERIALS CO,.LTD

Product: MLN-4760 305335-31-3
Price: US $2.00-5.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 100kg
Release date: 2025-06-30

305335-31-3, MLN-4760Related Search:

Pevonedistat MLN9708 MLN-8237

MLN-4760

L-Histidine, N-[(1S)-1-carboxy-3-methylbutyl]-3-[(3,5-dichlorophenyl)methyl]-

((S)-1-carboxy-2-(1-(3,5-dichlorobenzyl)-1H-imidazol-5-yl)ethyl)-L-leucine

inhibit,Angiotensin-converting Enzyme (ACE),MLN 4760,Inhibitor,MLN-4760,MLN4760

(2S)-2-{[(1S)-1-carboxy-2-{1-[(3,5-dichlorophenyl)methyl]-1H-imidazol-5-yl}ethyl]amino}-4-methylpentanoic acid

ACE2 Inhibitor, MLN-4760

MLN-4760 Chemical Structure

MLN-4760 ，S8940

305335-31-3