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Licofelone

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Catalog No. T6568Cas No. 156897-06-2
Alias ML-3000

Licofelone (ML-3000) is a dual COX/LOX inhibitor potentially for treating osteoarthritis, acting as both an analgesic and anti-inflammatory. By inhibiting 5-LOX, it may reduce the gastrointestinal toxicity associated with other non-steroidal anti-inflammatory drugs, which only inhibit COX (cyclooxygenase).

Licofelone

Licofelone

😃Good
Purity: 99.25%
Catalog No. T6568Alias ML-3000Cas No. 156897-06-2
Licofelone (ML-3000) is a dual COX/LOX inhibitor potentially for treating osteoarthritis, acting as both an analgesic and anti-inflammatory. By inhibiting 5-LOX, it may reduce the gastrointestinal toxicity associated with other non-steroidal anti-inflammatory drugs, which only inhibit COX (cyclooxygenase).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$39In StockIn Stock
10 mg$64In StockIn Stock
25 mg$128In StockIn Stock
50 mg$197In StockIn Stock
100 mg$293In StockIn Stock
200 mg$437-In Stock
500 mg$693-In Stock
1 mL x 10 mM (in DMSO)$43In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.25%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Licofelone (ML-3000) is a dual COX/LOX inhibitor potentially for treating osteoarthritis, acting as both an analgesic and anti-inflammatory. By inhibiting 5-LOX, it may reduce the gastrointestinal toxicity associated with other non-steroidal anti-inflammatory drugs, which only inhibit COX (cyclooxygenase).
Targets&IC50
5-LOX:0.18 μM, COX:0.21 μM
In vitro
The dual COX/5-LOX inhibitor licofelone triggers apoptosis in a dose- and time-dependent manner in HCA-7 colon cancer cells.?Induction of apoptosis was related to the recruitment of the intrinsic mitochondrial apoptotic pathway, as shown by loss in mitochondrial membrane potential, cytochrome c release, caspase-9 and 3 activation and poly-(ADP-ribose)polymerase-1 cleavage.?Moreover, licofelone induced the cleavage of the full-length p21(Bax) into p18(Bax), a more potent inducer of the apoptotic process than the uncleaved form.?Pre-treatment of HCA-7 cells with the pan-caspase inhibitor z-VAD-fmk significantly blocked licofelone-induced apoptosis, confirming that this process occurred primarily in a caspase-dependent pathway.?Licofelone was able to affect the arachidonic acid (AA) cascade, as it blocked the activity of 5-LOX and COX enzymes, and it induced, through the phosphorylation of cytoplasmic phospholipase A(2) (cPLA(2)), the release of unesterified AA from HCA-7 membrane phospholipids.[1]
SynonymsML-3000
Chemical Properties
Molecular Weight379.88
FormulaC23H22ClNO2
Cas No.156897-06-2
SmilesCC1(C)Cc2c(c(c(CC(O)=O)n2C1)-c1ccc(Cl)cc1)-c1ccccc1
Relative Density.1.23 g/cm3
Storage & Solubility Information
Storagestore at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 25 mg/mL (65.81 mM), Sonication is recommended.
Ethanol: 10 mg/mL (26.32 mM), Sonication is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble) (< 1 mM)
In Vivo Formulation
10% DMSO+90% Corn Oil: 2 mg/mL (5.26 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
H2O/Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.6324 mL13.1621 mL26.3241 mL131.6205 mL
Ethanol/DMSO
1mg5mg10mg50mg
5 mM0.5265 mL2.6324 mL5.2648 mL26.3241 mL
10 mM0.2632 mL1.3162 mL2.6324 mL13.1621 mL
20 mM0.1316 mL0.6581 mL1.3162 mL6.5810 mL
DMSO
1mg5mg10mg50mg
50 mM0.0526 mL0.2632 mL0.5265 mL2.6324 mL

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TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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