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Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $39 | In Stock | |
10 mg | $64 | In Stock | |
25 mg | $128 | In Stock | |
50 mg | $197 | In Stock | |
100 mg | $293 | In Stock | |
200 mg | $437 | In Stock | |
500 mg | $693 | In Stock | |
1 mL x 10 mM (in DMSO) | $43 | In Stock |
Description | Licofelone (ML-3000) is a dual COX/LOX inhibitor potentially for treating osteoarthritis, acting as both an analgesic and anti-inflammatory. By inhibiting 5-LOX, it may reduce the gastrointestinal toxicity associated with other non-steroidal anti-inflammatory drugs, which only inhibit COX (cyclooxygenase). |
Targets&IC50 | 5-LOX:0.18 μM, COX:0.21 μM |
In vitro | The dual COX/5-LOX inhibitor licofelone triggers apoptosis in a dose- and time-dependent manner in HCA-7 colon cancer cells.?Induction of apoptosis was related to the recruitment of the intrinsic mitochondrial apoptotic pathway, as shown by loss in mitochondrial membrane potential, cytochrome c release, caspase-9 and 3 activation and poly-(ADP-ribose)polymerase-1 cleavage.?Moreover, licofelone induced the cleavage of the full-length p21(Bax) into p18(Bax), a more potent inducer of the apoptotic process than the uncleaved form.?Pre-treatment of HCA-7 cells with the pan-caspase inhibitor z-VAD-fmk significantly blocked licofelone-induced apoptosis, confirming that this process occurred primarily in a caspase-dependent pathway.?Licofelone was able to affect the arachidonic acid (AA) cascade, as it blocked the activity of 5-LOX and COX enzymes, and it induced, through the phosphorylation of cytoplasmic phospholipase A(2) (cPLA(2)), the release of unesterified AA from HCA-7 membrane phospholipids.[1] |
Alias | ML-3000 |
Molecular Weight | 379.88 |
Formula | C23H22ClNO2 |
Cas No. | 156897-06-2 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 25 mg/mL (65.81 mM), Sonication is recommended. Ethanol: 10 mg/mL (26.32 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) (< 1 mM) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/Ethanol/DMSO
Ethanol/DMSO
DMSO
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