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MLN-4760 ACE inhibitor

Name: MLN-4760
Brand: Selleck Chemicals
SKU: S8940
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S8940

MLN-4760 (compound 16) is a potent and selective inhibitor of human angiotensin-converting enzyme 2 (ACE2) with IC50 of 0.44 nM. This compound also inhibits bovine carboxypeptidase A (CPDA) with IC50 of 27 μM.

Chemical Structure

Molecular Weight: 428.31

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Quality Control

Batch: S894001 Water]86 mg/mL]false]Ethanol]10 mg/mL]false]DMSO]Insoluble]false Purity: 99.60%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.60

Related Targets	Adrenergic Receptor Estrogen/progestogen Receptor GPR Androgen Receptor Glucocorticoid Receptor RAAS Progesterone Receptor Opioid Receptor PGES THR
Other ACE Inhibitors	DX600

Solubility

In vitro
Batch:

Water : 86 mg/mL

Ethanol : 10 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Clear solution	5%ethyl alcohol 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (1.17mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clarified ethyl alcohol stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% ethyl alcohol 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (1.17mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear ethyl alcohol stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	428.31	Formula	C₁₉H₂₃Cl₂N₃O₄	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	305335-31-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(C)CC(C(=O)O)NC(CC1=CN=CN1CC2=CC(=CC(=C2)Cl)Cl)C(=O)O

Mechanism of Action

Targets/IC₅₀/Ki	ACE2 (Cell-free assay) 0.44 nM CPDA (Cell-free assay) 27 μM
In vitro	In vitro, conversion from angiotensin II to angiotensin-(1–7) by mouse ACE2 is blocked by MLN-4760 (10 μM). This compound inhibits both human and mouse ACE2 activity. In huMNCs, this chemical-B (an isomer of MLN-4760) detects 63% ACE2 with 28-fold selectivity over ACE. In huCD34+ cells, this compound-B detects 38% of ACE2 activity with 63-fold selectivity. In mu-heart and muMNCs, this chemical-B is 100- and 228-fold selective for ACE2, respectively. In muLin- cells, this compound-B detects 25% ACE2 activity with a pIC50 of 6.3. The racemic mixture and this chemical-A shows lower efficacy and poor selectivity for ACE2 in MNCs and mu-heart.
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 this compound.
References	[1] https://pubmed.ncbi.nlm.nih.gov/12358520/ [2] https://pubmed.ncbi.nlm.nih.gov/29066981/ [3] https://pubmed.ncbi.nlm.nih.gov/22777933/ [4] https://pubmed.ncbi.nlm.nih.gov/26851370/

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