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Purity: ≥98%
Lumiracoxib (formerly CGS-35189; COX-189; trade name Prexige), a non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 enzyme inhibitor with potential anti-inflammatory activity. It inhibits COX-2 with an IC50 and a Ki of 0.14 μM and 0.06 μM, and exhibits 515-fold selectivity for COX-2 over COX-1. Lumiracoxib has anti-inflammatory, analgesic and antipyretic activities comparable with diclofenac, the reference NSAID, but with much improved gastrointestinal safety. Lumiracoxib has an IC50 of 0.14 μm in COX-2-expressing dermal fibroblasts, but caused no inhibition of COX-1 at concentrations up to 30 μm.
| ln Vitro |
Purified COX-1 and COX-2 are inhibited by lumiracoxib, with Ki values of 3 μM and 0.06 μM, respectively. In experiments using human COX-1 transfected HEK293 cells, lumiracoxib exhibits an IC50 of 0.14 μM in COX-2-expressing dermal fibroblasts, but does not inhibit COX-1 at dosages up to 30 μM[1]. The IC50 values for Lumiracoxib in a human whole blood experiment are 0.13 μM for COX-2 and 67 μM for COX-1[1].
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| ln Vivo |
In a rat model, lumiracoxib (oral administration; 10 and 30 mg/kg; single dose) considerably reverses the established hyperalgesia, with a peak reversal of 58% observed three hours after delivery[1]. The weight-bearing disparity that is seen on days 14, 17, and 20 is greatly reduced by lumiracoxib (oral administration; 10 and 30 mg/kg; twice daily; from day 10 to day 20 following MRMT-1 cell injection). Static allodynia evaluated 90 minutes after the final administration is significantly reversed by repeated administration.Twenty days after MRMT-1 cell inoculation in rats, it dramatically diminishes the structural alterations seen by radiography[1].
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| Animal Protocol |
Animal/Disease Models: Rat model of bone cancer pain with injection of MRMT-1 tumor cells into one tibia[1]
Doses: 10 and 30 mg/ kg Route of Administration: Oral administration; 10 and 30 mg/kg; twice (two times) daily; from day 10 to day 20 following MRMT-1 cell injection Experimental Results: Had an effect on mechanical hyperalgesia in a model of bone cancer pain. |
| References |
[1]. Ronald Esser, et al. Preclinical pharmacology of lumiracoxib: a novel selective inhibitor of cyclooxygenase-2. Br J Pharmacol. 2005 Feb;144(4):538-50.
[2]. Alyson Fox, et al. Anti-hyperalgesic activity of the cox-2 inhibitor lumiracoxib in a model of bone cancer pain in the rat. Pain |
| Molecular Formula |
C15H13CLFNO2
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| Molecular Weight |
293.72
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| CAS # |
220991-20-8
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| Related CAS # |
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| SMILES |
O=C(O)CC1=CC(C)=CC=C1NC2=C(F)C=CC=C2Cl
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| InChi Key |
KHPKQFYUPIUARC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H13ClFNO2/c1-9-5-6-13(10(7-9)8-14(19)20)18-15-11(16)3-2-4-12(15)17/h2-7,18H,8H2,1H3,(H,19,20)
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| Chemical Name |
2-(2-((2-chloro-6-fluorophenyl)amino)-5-methylphenyl)acetic acid
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| Synonyms |
Lumiracoxib; COX-189; CGS-35189; CGS 35189; COX189; CGS35189; COX 189; trade name: Prexige.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4046 mL | 17.0230 mL | 34.0460 mL | |
| 5 mM | 0.6809 mL | 3.4046 mL | 6.8092 mL | |
| 10 mM | 0.3405 mL | 1.7023 mL | 3.4046 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.
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