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Licofelone (Synonyms: ML 3000)

Catalog No.GC16721

COX-1, COX-2 and 5-LOX inhibitor

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Licofelone Chemical Structure

Cas No.: 156897-06-2

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10mM (in 1mL DMSO)
$62.00
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5mg
$54.00
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50mg
$371.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

IC50: Inhibitor of COX-1, COX-2 and 5-LOX with IC50 values of 0.16 M, 0.37 M and 0.23 M respectively in human.

Licofelone (ML3000), developed by the German pharmaceutical company - Merckle GmbH, is a potent suppressor of both COX and LOX. As the first member of this new class of analgesic and anti-inflammatory drugs, Licofelone is suggested as a novel treatment for osteoarthritis (OA), the most common form of arthritis. [1]

In vitro: The 5-LOX and COX inhibitory effect of licofelone was firstly identified via bovine thromobocyte intact cell assay and intact bovine PMN leukocytes. Licofelone was also reported to inhibit PGE2 in a dose-dependent manner in human whole blood assay. Moreover, Licofelone was found to suppress in vitro generation of reactive oxygen species and to reduce release of elastase from PMN leukocytes. All above findings revealed that Licofelone had an inhibitory effect on COX-1/-2 and 5-LOX. [1]

In vivo: The pharmacodynamic properties of Licofelone were evaluated in various animal models and compared with those of commonly used NSAIDs. Based on studies from a rat model of incisional pain, orally administration of Licofelone had a longer duration of action and was more effective than indomethacin and zileuton. [1]

Clinical trials: Two double-blind phase-II studies had been conducted to detect the efficacy of licofelone in OA. In the first study, 107 patients were treated with different doses of licofelone or placebo for 4 weeks. It was reported that licofelone at 200 or 400 mg twice a day could significantly ameliorate the symptoms of OA. In the second study, licofelone at doses of 100, 200 and 400 mg was administered to 404 patients twice a day, WOMAC pain subscore showed a notable decrease of 37%, 40% and 42% respectively. Licofelone at 400 mg twice a day was found to cause adverse events including diarrhea and abdominal pain. [1]

Reference:
[1]Kulkarni SK and Singh VP.  Licofelone-a novel analgesic and anti-inflammatory agent. Curr Top Med Chem. 2007; 7(3): 251-63.

Chemical Properties

Cas No. 156897-06-2 SDF
Synonyms ML 3000
Chemical Name 2-[2-(4-chlorophenyl)-6,6-dimethyl-1-phenyl-5,7-dihydropyrrolizin-3-yl]acetic acid
Canonical SMILES CC1(CC2=C(C(=C(N2C1)CC(=O)O)C3=CC=C(C=C3)Cl)C4=CC=CC=C4)C
Formula C23H22ClNO2 M.Wt 379.88
Solubility ≥ 6.3mg/mL in DMSO with gentle warming Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 6 reference(s) in Google Scholar.)

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