Licofelone (Synonyms: ML-3000)

Name: Licofelone
Brand: MedChemExpress
SKU: HY-B1452
Rating: 4.5 (1 reviews)

Cat. No.: HY-B1452 Purity: 98.62%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC₅₀=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins.

For research use only. We do not sell to patients.

Licofelone Chemical Structure

CAS No. : 156897-06-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Licofelone:

Licofelone-d4 Get quote
Licofelone-d₆ Get quote

1 Publications Citing Use of MCE Licofelone

•Clin Nutr. 2023 Dec 30;43(2):453-467. [Abstract]

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All COX Isoform Specific Products:

View All Isoforms

COX COX-1 COX-2 COX-3

View All Lipoxygenase Isoform Specific Products:

View All Isoforms

5-LOX 12-LOX 15-LOX

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[3]

COX

0.21 μM (IC₅₀)

5-LOX

0.18 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	6 μM Compound: 3, ML3000	Inhibition of mPGES1 in IL1-beta treated human A549 cell microsomal membrane assessed as blockade of PGH2 to PGE2 conversion after 1 min Inhibition of mPGES1 in IL1-beta treated human A549 cell microsomal membrane assessed as blockade of PGH2 to PGE2 conversion after 1 min	[PMID: 19719242]
A549	IC₅₀	6.7 μM Compound: 3, ML3000	Inhibition of mPGES1 in IL1-beta treated human A549 cell microsomal membrane assessed as residual enzyme activity after 1 min by measuring PGE2 level using RP-HPLC method Inhibition of mPGES1 in IL1-beta treated human A549 cell microsomal membrane assessed as residual enzyme activity after 1 min by measuring PGE2 level using RP-HPLC method	[PMID: 19719242]
HeLa	IC₅₀	6 μM Compound: Licofelone	Inhibition of mPGES1 in human HeLa cells assessed as reduction in TNF-alpha induced PGE2 production preincubated for 2 hrs followed by TNF-alpha addition for 24 hrs by ELISA Inhibition of mPGES1 in human HeLa cells assessed as reduction in TNF-alpha induced PGE2 production preincubated for 2 hrs followed by TNF-alpha addition for 24 hrs by ELISA	[PMID: 27597418]
HT-29	IC₅₀	21.1 μM Compound: Licofelone	Cytotoxicity against COX-2 positive human HT-29 cells transfected with CD44v6shRNA assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against COX-2 positive human HT-29 cells transfected with CD44v6shRNA assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 24295787]
HT-29	IC₅₀	67 μM Compound: Licofelone	Cytotoxicity against COX-2 positive human HT-29 cells assessed as growth inhibition by CellTiter-96 AQueous assay Cytotoxicity against COX-2 positive human HT-29 cells assessed as growth inhibition by CellTiter-96 AQueous assay	[PMID: 24295787]
MCF7	IC₅₀	36.7 μM Compound: Licofelone	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs	[PMID: 21295381]
MDA-MB-231	IC₅₀	5.5 μM Compound: Licofelone	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs	[PMID: 21295381]
SW480	IC₅₀	68 μM Compound: Licofelone	Cytotoxicity against COX-2 negative human SW480 cells assessed as growth inhibition by CellTiter-96 AQueous assay Cytotoxicity against COX-2 negative human SW480 cells assessed as growth inhibition by CellTiter-96 AQueous assay	[PMID: 24295787]

In Vitro

The IC₅₀s of human thrombocyte COX and human 5-LO are 0.16 μM and 0.23 μM, respectively^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

379.88

Formula

C₂₃H₂₂ClNO₂

CAS No.

156897-06-2

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(O)CC1=C(C2=CC=C(Cl)C=C2)C(C3=CC=CC=C3)=C4N1CC(C)(C)C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (65.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6324 mL	13.1621 mL	26.3241 mL
5 mM	0.5265 mL	2.6324 mL	5.2648 mL
10 mM	0.2632 mL	1.3162 mL	2.6324 mL

View the 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.58 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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: ≥99.0%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (255 KB)

Handling Instructions (2659 KB)

References

[1]. Tavolari S, et al. Licofelone, a dual COX/5-LOX inhibitor, induces apoptosis in HCA-7 colon cancer cells through the mitochondrial pathway independently from its ability to affect the arachidonic acid cascade. Carcinogenesis. 2008 Feb;29(2):371-80. [Content Brief]

[2]. Alvaro-Gracia JM, et al. Licofelone--clinical update on a novel LOX/COX inhibitor for the treatment of osteoarthritis. Rheumatology (Oxford). 2004 Feb;43 Suppl 1:i21-5. [Content Brief]

[3]. Laufer SA, et al. (6,7-Diaryldihydropyrrolizin-5-yl)acetic acids, a novel class of potent dual inhibitors of both cyclooxygenase and 5-lipoxygenase. J Med Chem. 1994 Jun 10;37(12):1894-7. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.6324 mL	13.1621 mL	26.3241 mL	65.8103 mL
	5 mM	0.5265 mL	2.6324 mL	5.2648 mL	13.1621 mL
	10 mM	0.2632 mL	1.3162 mL	2.6324 mL	6.5810 mL
	15 mM	0.1755 mL	0.8775 mL	1.7549 mL	4.3874 mL
	20 mM	0.1316 mL	0.6581 mL	1.3162 mL	3.2905 mL
	25 mM	0.1053 mL	0.5265 mL	1.0530 mL	2.6324 mL
	30 mM	0.0877 mL	0.4387 mL	0.8775 mL	2.1937 mL
	40 mM	0.0658 mL	0.3291 mL	0.6581 mL	1.6453 mL
	50 mM	0.0526 mL	0.2632 mL	0.5265 mL	1.3162 mL
	60 mM	0.0439 mL	0.2194 mL	0.4387 mL	1.0968 mL

Licofelone Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Licofelone156897-06-2ML-3000ML3000ML 3000COXLipoxygenaseApoptosisCyclooxygenaseLOXInhibitorinhibitorinhibit

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Licofelone (Synonyms: ML-3000)

Customer Review

Other Forms of Licofelone:

Licofelone Related Antibodies

1 Publications Citing Use of MCE Licofelone

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All COX Isoform Specific Products:

View All Lipoxygenase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Licofelone Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Licofelone Related Classifications

Keywords:

Your Recently Viewed Products:

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