Licofelone
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.84%
- No. CAS: 156897-06-2
- Fòrmula: C23H22ClNO2
- Peso molecular:379.88
-
Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
Ferroptosis Compound Library
HY-L051
-
Lipid Metabolism Compound Library
HY-L091
-
Human Metabolite Library
HY-L123
-
Anti-Prostate Cancer Compound Library
HY-L124
-
Non-steroidal Anti-Inflammatory Compound Library
HY-L130
-
Metabolic Enzyme Compound Library
HY-L146
-
Cell Death Library
HY-L162
-
Multi-Target Compound Library
HY-L176
-
Radioprotector Library
HY-L178
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
Anti-Fibrosis Compound Library
HY-L185
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
-
Anti-Rheumatic Arthritis Compound Library
HY-L210
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Apoptosis Compound Library
HY-L003
-
Immunology/Inflammation Compound Library
HY-L007
-
Metabolism/Protease Compound Library
HY-L012
-
Anti-Cancer Compound Library
HY-L025
-
Clinical Compound Library
HY-L026
-
Anti-Aging Compound Library
HY-L034
Publications Citing Use of MedChemExpress (MCE) Licofelone
More
Actividad biológica
|
COX 0.21 μM (IC50) |
5-LOX 0.18 μM (IC50) |
|
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] |
Chemical Information
-
No. CAS 156897-06-2
-
Appearance Solid
-
Peso molecular 379.88
-
Fòrmula 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
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
Clin Nutr
2023 Dec 30;43(2):453-467. PMID: 38181523
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
-
Ficha de datos (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)
-
Instrucciones de manejo (2659 KB)
Referencias
[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
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.
| 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
HY-B1452 Related Classifications
Powered by Bioz