| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Licofelone targets cyclooxygenase (COX-1 and COX-2) and 5-lipoxygenase (5-LOX). It acts as a dual inhibitor, blocking the activity of both enzymes. COX enzymes are responsible for the production of prostaglandins, while 5-LOX is responsible for the production of leukotrienes. By inhibiting both enzymes, licofelone reduces the production of multiple inflammatory mediators, providing both anti-inflammatory and analgesic effects.
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| ln Vitro |
Licofelone's half-life against human 5-LO and human resting COX is 0.23 μM and 0.16 μM, respectively[3].
In vitro, Licofelone has been shown to inhibit COX-1, COX-2, and 5-LOX enzyme activities in a concentration-dependent manner. It inhibits the production of prostaglandins and leukotrienes in various cell types. Licofelone also has been shown to have antioxidant properties. The compound's anti-inflammatory effects have been demonstrated in various in vitro models. |
| ln Vivo |
In vivo, Licofelone has been shown to be effective in reducing inflammation and pain in animal models of arthritis. Clinical studies have demonstrated its efficacy in reducing pain and improving function in patients with osteoarthritis. Licofelone has been shown to have a lower incidence of gastrointestinal ulcers compared to traditional NSAIDs, which is attributed to its dual inhibition of COX and 5-LOX.
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| Enzyme Assay |
In vitro enzyme inhibition assays for Licofelone typically involve measuring the activity of COX-1, COX-2, or 5-LOX in the presence of varying concentrations of the compound. The enzyme is incubated with its substrate and Licofelone, and the production of the product is measured. The IC50 value for inhibition of the enzyme is determined from dose-response curves. The selectivity of Licofelone for COX and 5-LOX over other enzymes can be assessed.
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| Cell Assay |
In vitro cell-based studies with Licofelone typically involve cultured inflammatory cells, such as macrophages or synoviocytes. Cells are treated with Licofelone at various concentrations in the presence or absence of inflammatory stimuli. The production of prostaglandins and leukotrienes is measured by ELISA. The effect of Licofelone on cytokine production and cell viability can also be evaluated.
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| Animal Protocol |
In vivo animal studies with Licofelone are typically conducted in rodent models of arthritis, such as the adjuvant-induced arthritis model or the collagen-induced arthritis model. The compound is administered orally. The effect of Licofelone on paw swelling, joint inflammation, and pain is assessed. The compound's effect on gastrointestinal toxicity is also evaluated. Pharmacokinetic studies are performed by measuring compound concentrations in plasma and tissues.
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
Known human metabolites of ricolone include ricolone M4, ricolone M2, and (2S,3S,4S,5R)-6-[2-[2-(4-chlorophenyl)-6,6-dimethyl-1-phenyl-5,7-dihydropyrrolidine-3-yl]acetyl]oxy-3,4,5-trihydroxyoxacyclohexane-2-carboxylic acid. The pharmacokinetic properties of Licofelone have been studied in preclinical and clinical settings. Following oral administration, the compound is absorbed from the gastrointestinal tract. Licofelone is metabolized in the liver. The elimination half-life is approximately 8-12 hours. Licofelone is excreted in the urine and feces primarily as metabolites. |
| Toxicity/Toxicokinetics |
The toxicity profile of Licofelone has been evaluated in clinical studies. The most common adverse effects are mild and include gastrointestinal upset, headache, and dizziness. Licofelone has been shown to have a lower incidence of gastrointestinal ulcers compared to traditional NSAIDs. However, the compound can still cause gastrointestinal irritation and bleeding. Licofelone should be used with caution in patients with a history of gastrointestinal disease.
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| References |
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| Additional Infomation |
Ricofenone (ML3000), co-developed by German pharmaceutical company Merckle GmbH and EuroAlliance partners Alfa Wassermann and Lacer, is a dual COX/LOX inhibitor and the first of its kind. It is currently being evaluated for the treatment of osteoarthritis (OA), the most common type of arthritis. Although a Phase III clinical trial in OA patients has been successfully completed, a regulatory application date has not yet been announced. Indications: For the treatment of osteoarthritis. Mechanism of Action: Ricofenone reduces the levels of inflammatory prostaglandins and leukotrienes by simultaneously inhibiting 5-LOX and COX. Pharmacodynamics: Ricofenone belongs to a new class of dual-action anti-inflammatory drugs called COX/LO inhibitors. These drugs simultaneously inhibit cyclooxygenase (COX) and 5-lipoxygenase (LO).
Licofelone (ML3000) is a dual inhibitor of COX and 5-LOX that was developed for the treatment of osteoarthritis and other inflammatory conditions. It has a favorable gastrointestinal safety profile compared to traditional NSAIDs. Licofelone is not widely approved as a drug and is not commercially available in many countries. The compound continues to be an area of research for its potential therapeutic applications. |
| Molecular Formula |
C23H22CLNO2
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|---|---|
| Molecular Weight |
379.87928
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| Exact Mass |
379.133
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| CAS # |
156897-06-2
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| Related CAS # |
Licofelone-d6;1178549-81-9
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| PubChem CID |
133021
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
539.7±50.0 °C at 760 mmHg
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| Melting Point |
162-163ºC
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| Flash Point |
280.2±30.1 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.627
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| LogP |
6.73
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
537
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UAWXGRJVZSAUSZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H22ClNO2/c1-23(2)13-19-22(15-6-4-3-5-7-15)21(16-8-10-17(24)11-9-16)18(12-20(26)27)25(19)14-23/h3-11H,12-14H2,1-2H3,(H,26,27)
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| Chemical Name |
(6-(4-Chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl)acetic acid
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| Synonyms |
ML-3000 ML 3000 ML3000.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~65.81 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00671593 | Terminated | Biological: House Dust Mite Biological: Diluent |
Atopic Asthma Healthy |
John Sundy | 2006-10 | Phase 1 |
| NCT03521713 | Unknown status | Drug: EPORON Drug: EPREX |
Anemia of Chronic Kidney Disease | Dong-A ST Co., Ltd. | 2016-03-01 | Phase 3 |
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