Cat. No.: HY-B1452

Licofelone

(Synonyms: ML-3000)

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

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.

Purity: 99.84%
CAS No.: 156897-06-2
Formula: C₂₃H₂₂ClNO₂
Molecular Weight:379.88

Storage:

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

Licofelone Chemical Structure

CAS No.: 156897-06-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[3]

COX

0.21 μM (IC₅₀)

5-LOX

0.18 μM (IC₅₀)

All COX Isoforms :

All Lipoxygenase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	EC₅₀	0.1 μM Compound: Licofelone	Inhibition of mPGES1 in human A549 cells assessed as reduction in PGE2 production Inhibition of mPGES1 in human A549 cells assessed as reduction in PGE2 production	[PMID: 27597418]
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]
PMNL	IC₅₀	0.18 μM Compound: 3e	Inhibition of 5-lipoxygenase in bovine PMNL cell assay. Inhibition of 5-lipoxygenase in bovine PMNL cell assay.	[PMID: 8021931]
RBL-1	IC₅₀	3.6 μM Compound: Licofelone, ML-3000	Inhibition of 5-LOX in rat RBL1 cells assessed as reduction in LTB4 production Inhibition of 5-LOX in rat RBL1 cells assessed as reduction in LTB4 production	[PMID: 22380511]
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.

Chemical Information

CAS No. 156897-06-2
Appearance Solid
Molecular Weight 379.88
Formula C₂₃H₂₂ClNO₂
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
Synonyms

ML-3000
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

Publications (1)

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Clin Nutr

Adaptive metabolic response to short-term intensive fasting. [Abstract]

2023 Dec 30;43(2):453-467. PMID: 38181523

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

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Licofelone

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Ferroptosis Compound Library

Lipid Metabolism Compound Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Non-steroidal Anti-Inflammatory Compound Library

Metabolic Enzyme Compound Library

Cell Death Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Licofelone

All COX Isoforms

All Lipoxygenase Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Licofelone

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Ferroptosis Compound Library

Lipid Metabolism Compound Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Non-steroidal Anti-Inflammatory Compound Library

Metabolic Enzyme Compound Library

Cell Death Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Licofelone

All COX Isoforms

All Lipoxygenase Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Licofelone Related Classifications

HY-B1452 Related Classifications